대한약학회:학술대회논문집 (Proceedings of the PSK Conference) (Proceedings of the PSK Conference)
대한약학회 (The Pharmaceutical Society of Korea)
- 기타
과학기술표준분류
- 보건의료 > 의약품/의약품개발
대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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The cause of Huntington's disease (HD) is a pathological expansion of the polyglutamine domain within the N-terminal region of huntingtin. Neuronal aggregates composed of mutant huntingtin within certain neuronal populations are a characteristic hallmark of HD. Because tissue transglutaminase (tTG) cross-links proteins into aggregates and polypeptide-bound glutamines are primary determining factors for tTG-catalyzed reactions, it has been hypothesized that tTG may contribute to the formation of aggregates. (omitted)
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Cerebral ischemia, the most prevalent form of clinical stroke, is a medical problem of the first magnitude. Substantial efforts are being made to develop drugs which will protect the brain from the neurodegeneration that follows ischemic stroke. However, no medical treatment is currently approved for the treatment of stroke to reduce brain infarction or neurological disability beyond tissue plasminogen activator. (omitted)
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Design and Combonatorial Synthesis of Selenoflavonoids and Indole Compounds for Neuroprotective DrugAs recent as 10 years ago, a method of developing new medicine was developed by a new compounding method moving away from an existing one. Combinatorial chemistry made it easier to combine various kinds of compounds in a very short time and with little effort from existing methods. Through combinatorial chemistry, a number of compounds were synthesized using HTS(High Throughput Screening), with many reports reaching a clinical stage in search of new candidate material. (omitted)
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Excitatory amino acid (EAA) receptor, particularly NMDA receptor, are now known to be one of major transmitter receptors involved in synaptic excitation. Excessive release of EAA neurotransmitter, glutamate, is an important causative factor in the neurodegenerative processes and can cause neuronal damage and cell death. This excitotoxicity has been shown to be
$Ca^{++}$ dependent. (omitted) -
Much of the recent increase in research on nicotinic ligands has been motivated by a growing body of evidence that nicotinic cholinergic pharmacology plays a role in disorder associated with deficits of cognitive function in humans. The importance of developing novel nicotinic ligands as potential therapeutics is emphasized by studies with nicotine itself that have demonstrated many useful CNS and cognitive effects in various disorders such as dementia. (omitted)
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p43 is a protein with complex biological activities. It is first found as a protein associated with macromolecular tRNA synthetase complex. Within this complex, p43 specifically interacts with arginyl-tRNA synthetase to help the substrate tRNA binding to the enzyme. It is also necessary for the cellular stability of arginyl-tRNA synthetase and the molecular association of a few complex-forming tRNA synthetases. (omitted)
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T cell activation is initited by the interaction of T cells with antigen-presenting cells (APCs) in the context of peptide antigen. Initial conjugates are formed by binding between lymphocyte-associated antigen-l (LFA-l, also known as CD11a-CD18) and intercellular adhesion molecule-l (ICAM-1), or CD2 and LFA-3, or other pairs of interactive proteins. (omitted)
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IL-18 has been found to have multiple effects upon various cells involved in tumor immunology. Here, we discuss opposite effects of IL-18 in tumor immunology. IL-18 has been shown that it has significant anti-tumor effects, which are mediated by T cells and NK cells, in a manner similar to IL-12. First, we investigated the evaluation of the effects of the systemic administration of IL-18 in combination with B7-1 (CD80) against murine B16 melanoma in vivo. (omitted)
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In the past it was thought that autoimmunity is mediated by antibodies and immune complexes. It has now become clear that many diseases, especially tissue specific, are T cell mediated or at least T cell dependent. The pathogenesis of cell-mediated autoimmune diseases, such as multiple sclerosis, uveitis, diabetes, arthritis, and others, is thought to be in a large measure driven by interferon-gamma-producing antigen-specific T cells polarized toward the Th1 phenotype. (omitted)
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The purposes of this study were to evaluate the population pharmacokinetics of levosulpiride and terbinafine according to several pharmacokinetic models and to investigate the influence of characteristics of subjects such as age, body weight, height and serum creatinine concentration on the pharmacokinetic parameters of levosulpiride and terbinafine, respectively. (omitted)
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In recent days, the bioequivalence(BE) study of domestic drugs on original drug are quite, activated in Korea. This BE study provide not only the bioequivalence of test and reference drug but also produce the population pharmacokinetic(PK) parameters in normal healthy Korean. The BE study can also make it possible to establish a PK/PD model of the drug when the additional pharmacodynamic(PD) data are available. (omitted)
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Sample size calculations play an important role in bioequivalence trials. In almost all clinical trials sample size is determined by considering power under the alternative hypothesis. The alternative hypothesis is the hypothesis that we wish to prove with experiments. Hence, in bioequivalence trials the alternative hypothesis is that two formulations are bioequivalent, while the null hypothesis is that the two formulations are not bioequivalent. (omitted)
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Virtually every state in US has adopted laws and regulations that mandate the generic substitution of brand-named prescription drugs in order to reduce sky-rocketing drug costs. In the late 1970s, many state governments began to recognize the need of generic substitution and requested Food and Drug Administration (FDA) to consult with this issue. FDA did consult which drugs were interchangeable each other based upon the available scientific and experimental evidences given to the agency along with New Drug Application (NDA) and Abbreviated New Drug Application (ANDA). (omitted)
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Selenium is an ultra trace essential element for the normal functioning body because of forming the active center of redox enzymes such as four kinds of glutathione peroxidases (GPx), thioredoxin reductase (TR) and 5'-iodothyronine deiodinase. However, the adequate range between deficient and excessive levels is very narrow. (omitted)
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1. Standard and regulations for functional food evaluation cases form overseas (1) Japan For food function indication, Food Nutrition Improvement Act was amended in September 1991 and they managed functional food after setting specific health food in one of classification of special functional foods. For manification of raw material usage, the classification of health functional foods was performed by their application on: the control of internal organ status, cholesterol, blood pressure, mineral absorption, and prevention of dental caries. (omitted)
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The term allergy was originally defined by Clemens Yon Pirquet as ‘an altered capacity of the body to react to foreign substance’, which was an extremely board definition that included all immunological reactions. Allergy is now defined in a much more restricted manner as ‘disease following an immune response to an otherwise innocuous antigen’. Allergy is a member of a class of immune responses that have been termed hypersensitivity reactions; these are harmful immune responses that produce tissue injury and may cause serious disease. (omitted)
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Use of functional foods for health promotion and disease prevention has increased over the years. The reasons for consuming functional foods are to decrease the risk of certain diseases and age-related changes along with enhancing physical performance. Unfortunately, some functional foods lack sufficient scientific evidences to support health effects at the present. (omitted)
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The epithelial cells that form a barrier lining the lung airway are key regulators of neutrophil trafficking into the airway lumen in a variety of lung inflammatory diseases. Although the lipid mediator leukotriene B
$_4$ (LTB$_4$ ) is known to be a principal chemoattractant for recruiting neutrophils to inflamed sites across the airway epithelium, the precise signaling mechanism involved remains largely unknown. (omitted) -
The epidermal growth factor (EGF) is an important signaling ligand for the mitogenesis of many cells. The EGF receptors use signaling molecule multicomplexes and dynamic protein networks for the transmission and amplification of the signals as well as for the regulation of the cellular responses. EGF signaling has been reported to be enhanced in various tumors by the overexpressed EGF receptor and/or the mediators such as phospholipase C-
$\gamma$ 1(PLC$\gamma$ 1). (omitted) -
Phospholipids function as major components of biological membranes as well as precursors of biologically active lipid messengers. It is well known that arachidonic acid attached at the sn-2 position of phosphoglycerides serves as a precursor of prostaglandins and leukotrienes. Recently, it has been recognized that lysophospholipids such as lysophosphatidic acid, sphingosine 1-phosphate, lysophosphatidylserine and monoglyceride also function as lipid messengers with a variety of biological activities. (omitted)
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Biosynthsis of prostaglandin E2 (PGE2), the most common prostanoid with potent and diverse bio-activities, is regulated by three sequential enzymatic steps composed of phospholipase A2, cyclooxygenase (COX), and prostaglandin E synthase (PGES). Recently, three distinct PGESs have been identified; two of them are membrane-bound enzymes, mPGES-1 and mPGES-2, and the third one is a cytosolic enzyme, cPGES. (omitted)
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One of the most frequent defects in human cancer is the uncontrolled activation of the ras-signaling pathways. Elevated p21 ras expression is associated with tumor aggressiveness in breast cancer including the extent of invasion into fat tissues. infiltration into lymphatic vessels and tumor recurrence, We demonstrate that H-ras, but not N-ras, upregulates matrix metalloproteinase(MMP)-2 expression and induces invasive phenotype in MCF10A human breast epithelial cells. (omitted)
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The purpose of this study is to investigate the effect of mucosal vaccine delivery vehicles and adjuvants on the local and systemic antibody responses following mucosal immunization of mice with hepatitis B surface antigen (HBsAg). Mice were immunized on days 0 and 21 by administration of hepatitis B surface antigen B (HBsAg) into the vagina. HBsAg was delivered in saline or poloxamer(Pol)-based vehicle containing mucoadhesive polycarbophil (PC). (omitted)
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Bradykinin modulates the sympathetic system in various ways. It can stimulate sympathetic neurotransmission directly through presynaptic receptors (Llona et al., 1991) and indirectly via its hypotensive or nociceptive effects which activate central and ganglionic mechanisms (Kuo and Keeton, 1991; Dray et al., 1988). However, it has been found that bradykinin can also liberate prostaglandins in peripheral tissues, thereby attenuating the release of catecholamines(Starke et al., 1977). (omitted)
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Kim, Mi-Jeong;Jung, Yi-Sook;Kim, Sun-Ok;Lee, Dong-Ha;Lim, Hong;Yi, Kyu-Yang;Yoo, Sung-Eun;Lee, Soo-Hwan;Baik, Eun-Joo 131
A benzopyranyl derivative, KR32158, synthesized as a plausible KATP opener, has been shown to exert cardioprotective effect in vivo myocardial infarction model. Myocardial ischemia, induced by oxidative stress, mental stress and fever, result in artheroscleosis, myocardial infarction and hypertrophy. In this study, we investigated in vitro effect of KR32158 by determining whether KR32158 produce cardioprotective effect against oxidative stress-induced death in heart-derived H9c2 cells. (omitted) -
Hangover is associated with ethanol metabolism in body after the ingestion of an alcoholic beverage. Especially. The metabolism in liver is forcused by many researcher because, alcohol (approximately 90%) is metabolized by the liver. Ethanol metabolism in liver involves both liver alcohol dehydrogenase(ADH) which actalyzes the oxidation of ethanol to acetaldehyde, and liver aldehyde dehydrogenase(ALDH) which metabilized rapidly acetaldehyde, product of ethanol oxidation, to acetate. (omitted)
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Alzheimer's disease (AD) is a neurodegenerative disorder characterized by the progressive deterioration of cognition and memory in association with widespread neuronal loss. AD is supposed to be very often associated with missense mutation located on homologous protein Presenilin (PS1) and (PS2). Up to now, the molecular mechanisms underlying the role of the gene mutation in AD still remain unclear. (omitted)
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Moon, C.K.;Jung, A.Y.;Kim, M.H.;Lee, Y.H.;Chae, S.H.;Kim, K.S.;Jo, Y.Y.;Kim, M.H.;Moon, K.S. 157
A newly synthesized thiazolodinedione derivative, CKD-501, was confirmed to have antihyperglycemic effect in in vivo study. The present study was undertaken to investigate the effect of CKD-501 on glucose transport and its stimulating mechanism in L6-myotubes. L6-myoblasts were cultured and differentiated to myotubes by reducing serum concentration in media from 10% to 2%. (omitted) -
Endosulfan is one of the organochlorine pesticides, well-known endocrine disruptors (EDs). Many EDs show the estrogenic effect. Estrogen is a group of hormones that play an important role in mammary gland function and implicated in mammary carcinogenesis. In the present study. using mouse mammary gland organ culture (MMOC) system. we studied the the effects of endosulfan on nodule like alveolar lesion (NLAL) formation in the mouse mammary gland development. (omitted)
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Shin JaeHo;Moon HyunJu;Kim TaeSung;Lee SuJung;Kang IlHyun;Kim InYoung;Bae Hoon;Ryu SungYeoul;Whang SungJo 187
The aims of present study were to compare the effects of in utero exposure to diethylstibestrol (DES), di(n-butyl)phthalate (DBP) and flutamide on the development of reproductive organs and to investigate the specific mechanisms of these abnormalities in the male reproductive system.During gestation days 10-19, pregnant Sparague-Dawley (SD) female rats were administered orally with corn oil (control), DES (25, 50, or 100${\mu}$ /kg/day), (omitted) -
Chronic inflammatory processes are associated with pathology of Alzheimer's disease(AD). The expression of both cyclooxygenase-2(COX-2) and phospholipase A2(PLA2) appears to be strongly activated during AD, indicating the importance of inflammatory gene pathways as a response to brain injury. Stimulation of heterotrimeric G protein-coupled receptors including muscarinic receptors activates cytosolic PLA2 and receptor-mediated activation of PLA2 generates free fatty acids (i.e., arachidonic acid). (omitted)
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The effect of radio- and chemotherapy for cancer are excellent, but their toxicities to normal tissue and organ of the body is relatively strong, which leads secondary side effect to patients during therapies. Particularly, due to the response for bone marrow suppression such as agranulocytosis limits the therapy periods and dose of drugs, new drug development that reproduces lymphocytes has been focused. (omitted)
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Oh, Mi-Jung;Park, Mi-Ja;Lee, Ji-Yeon;Park, Ji-Woo;Lee, Na-Gyong;Jung, Sung-Yun;Kim, Dae-Kyong 220
Bacterial infection is a very complex process in which both pathogens and host cells play crucial roles, and the host cells undergo drastic changes in their physiology, releasing various proteins in response to the pathogenic infection. Human airway epithelial surface serves as a first line of defense against microorganisms and the external environment. It is well known that bronchial epithelial cells secrete various chemokines and cytokines such as IL-6 and IL-8 to cope with various respiratory pathogens. (omitted) -
With the aim of obtaining the early bone regeneration efficacy, poly (L-lactide) particulates were developed as a long-term drug carrier system.Biodegradable microparticulates have been used extensively as drug delivery devices. However, problems like poor encapsulation efficiencies of the drugs and complicated fabrication process are still remained to be solved. (omitted)
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Lee, Jee-Hwan;Cho, Jung-Ah;Ki, Chan-Young;Son, Yeon-Kyoung;Park, Jeong-Hill;Park, Man-Ki;Han, Yong-Nam 318
The current study was performed to observe the effects of Panax ginseng (PG) and P. quinquefolium (PQ) on hemodynamics such as blood flow rate (BF), blood flow velocity (BV), heart rate (HR), systolic blood pressure (SBP), and diastolic blood pressure (DBP) and body temperature (BT) in healthy young men. This is a randomized, single-blind study observed during 6 hrs after orally single administration of PG and PQ groups. (omitted) -
Lee, Tai-Sang;Min, Young-Sil;Choi, Tae-Sik;Sim, Sang-Soo;Shin, Yong-Kyoo;Lee, Moo-Yeol;Sohn, Uy-Dong 117.1
We investigated whether experimental esophagitis and IL-1$\beta$ could induce the activation of MAP kinases in esophageal smooth muscle. With two models of experimental esophagitis, we assessed the activity of p38 MAP kinase, p44/42 MAP kinase and JNK. In feline acute experimental esophagitis, immunoblotting of normal and esophagitis-induced smooth muscle with each types of MAP kinase antibodies revealed the slight increase of phosphorylated form of p38 MAP kinase, especially in membrane fraction. (omitted) -
Sample size calculations plays an important role in a bioequivalence trials and is determined by considering power under the alternative hypothesis. The regulatory guideline recommends that
$2{\times}2$ crossover design is conducted and raw data is log-transformed for statistical analysis. In this paper, we discuss the sample size calculation in$2{\times}2$ crossover design with the log-transformed data. -
A growing body of scientific research indicates that man-made chemicals (xenobiotics) may interfere with the normal functioning of endocrine, or hormone systems. These endocrine disruptors may cause a variety of problems with development, behavior, and reproduction. Amongst the xenobiotics the World Health Organization classed 2, 3, 7, 8-TCDD as a "known" human carcinogen. (omitted)
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This study was undertaken to assess overall effects of bisphenol A, a monomer widely used in manufacturing polycarbonate plastics or epoxy resin, exposure on immune system of mice. For in vitro evaluation, serial concentration of SPA was added into culture of various immune cells from normal female ICR mice, and for in vivo or ex vivo assessment, mice were orally exposed to BPA dissolved in olive oil as doses of 500, 1000, 2000 mg/g b.w. for acute expose or 100, 500, 1000 mg/kg/day b.w. 5days a week for subacute exposure. (omitted)
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Nuclear factor-
${\kappa}{B}$ (NF-${\kappa}{B}$ ) belongs to a group of homodimers and heterodimers of Rel/NF-${\kappa}{B}$ proteins that bind to DNA target sites, where they directly regulate gene transcription. The activation of NF-${\kappa}{B}$ has been shown to mediate inflammation and suppress apoptosis. Activated NF-${\kappa}{B}$ has been found n various inflammatory diseases such as rheumatoid arthritis, Atherosclerosis, asthma, nflammatory bowel disease, and Helicobacter pylori-associated gastritis and associated with cancer, cachexia, diabetes, euthyroid sick syndrome, and AIDS. (omitted) -
The alkylphenols, chlorophenols and bisphenol A were determined by gas chromatography/mass spectrometry-selected ion monitoring (GC/MS-SIM) mode followed by two work-up methods for comparison; isoBOC derivatization method and TBDMS derivatization method. Eleven phenols in paper samples were extracted with acetonitrile. (omitted)
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Diabetes is complex in nature but it gets further complicated in associating with number of other diseases like hypertension, ratinal disintegration, renal failure and many others. The latest addition to diabetic-complication is its association with bone degeneration disease:osteoporosis, which is a form of bone loss. In both the types of primary diabetes, the insulin dependent diabetes militus (IDDM) as well in insulin independent diabetes millitus (IIDM) the glucose metabolism is altered. (omitted)
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Human tumor necrosis factor-alpha (TNFa) is a key pro-inflammatory cytokine produced by activated monocytes and macrophage as a part of the self-defence machinery. TNF-a converting enzyme (TACE) is the metalloproteinase that processes the membrane bound precursor of TNFa to the soluble component. (omitted)
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Adrenal medullary chromaffin cells secrete catecholamines in response to nicotinic agonists (Douglas & Rubin. 1961; Wakade, 1981; Amy & Kirshner, 1982). Several types of voltage-dependent Ca2+ channels are present on adrenal chromaffin cells, but the role of each type in the catecholamine secretion process remains controversial. (omitted)
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The therapeutic potential of currently available antiarrhythmic drugs is limited by their tendency to induce proarrhythmic and extracardiac side effects. An ideal antiarrhythmic agent would selectively prolong the action potential duration more in extraordinarily depolarized cardiac myocytes than in normal cells. and show tissue selectivity. Voltage-gated K+ (Kv) channels represent a structurally and functionally diverse group of membrane proteins. (omitted)
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The purpose of this study is to investigate the prevalence of resistance to macrolide, lincosamide, streptogramin and ketolide antibiotics in Korea. The antibiotic susceptibility test was performed to the macrolide erythromycin, clarithromycin, azithromycin, josamycin, the lincosamide clindamycin, the streptogramin synercid and the ketolide ABT -773 against 337 clinical Staphylococcus aureus(SAU). Coagulase-negative Staphylococci (CNS) and Enterococci isolates exhibited an average percentage of 64%, 56%, and 81 % of resistance to erythromycin, respectively.
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Lee, Sang-Kyu;Lee, Jae-Ick;Jahng, Young-Dong;Chang, Hyeun-Wook;Lee, Eung-Seok;Kim, Dong-Hyun;Jeong, Tae-Cheon 127.2
Rutaecarpine is an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa. In addition to its traditional use in treatment of gastrointestinal disorders, rutaecarpine has recently been characterized to have anti-inflammatory activity through cyclooxygenase-2 inhibition. More recently, to develop rutaecarpine as an anti-inflammatory agent, total synthesis of rutaecarpine has successfully been established in our group. (omitted) -
Oh, Tae-Young;Kim, Ju-Mi;Ahn, Byoung-Ok;Kim, Won-Bae;Park, Eun-Joo;Kim, Yong-Seok;Lee, Zee-Won;Ha, Kwon-Soo 129.1
Alcohol, Helicobacter pylori, stress and NSAIDs-activated neutrophils all produce reactive oxygen species (ROS), which play an important role in gastric mucosal damage. Eupatilin is an active component of Artemisia asiatica possessing cytoprotective effect. The effect of eupatilin on the production of ROS and cellular damage in AGS and ECV304 cells were evaluated to prove the cytoprotective action against the above mentioned gastric mucosal cell damages. (omitted) -
Jeong, Mi-Young;Shin, Chang-Yell;Sohn, Jin-Bup;Lee, In-Ki;Son, Mi-Won;Bae, Cheol-Jun;Byun, Jong-Soo;Kim, Dong-Sung;Kim, Soon-Hae 129.2
Recently. it has been known that NADPH-dependent isocitrate dehydrogenase (IDPc) involves in the obesity through production of NADPH, an important cofactor. DA-11004 is a synthetic potent IDPc inhibitor that$IC_{50}$ for IDPc is 1.49$\mu\textrm{M}$ (0.9$\mu$ g/ml). The purpose of this study was to evaluate the effects of DA-11004 on the high fat high sucrose (HF)-induced obesity in C57BL/6 mice. (omitted) -
The metabolism of a novel anticancer agent 1-{3- [3-(4-Cyano -benzyl)-3H-imidazol-4-yl]-propyl }-3-(6-methoxy-pyridin-3-yl)-1-(2-trifluoromethyl-benzyl)-thiourea (YH3945) were investigated in the Sprague-Dawley rat after single oral and i.v. administration of [14C]-YH3945. Bile, feces, urine and plasma were collected and analyzed by an HPLC system equipped with multiple detectors. (omitted)
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The present study was undertaken to examine the hypothesis that
$\mu$ -opioid receptors play a crucial role in behavioral sensitization to nicotine using$\mu$ -opioid receptor knockout mice. All mice were treated acutely or repeatedly with nicotine 0.05 mg/kg twice daily for 7 consecutive days. The mice were challenged with nicotine on day 11. And locomotor activity was measured for 30min. (omitted) -
Shin, Chang-Yell;Jeong, Mi-Young;Sohn, Jin-Bup;Lee, In-Ki;Son, Mi-Won;Bae, Cheol-Jun;Byun, Jong-Soo;Kim, Dong-Sung;Kim, Soon-Hae 130.3
The biological effects of NADPH-dependent isocitrate dehydrogenase (IDPc) inhibitor. DA-11004, was examined in obese zucker rats or streptozotocin-induced diabetic SD rats. Diabetes was induced by injection of streptozotocin (50mg/kg) dissolved in citrate buffer (pH 4.8) into the tail vein and induction of diabetes was confirmed by the measurement of the tail blood glucose level at 48h. DA-11004 (30mg/kg, po) was injected for successive 7days and significantly reduced the plasma glucose in streptozotocin-induced diabetic rats (P<0.05). (omitted) -
Novel trans-ditrifluoroacetato, malonato-1, 4-butanediamine Pt(IV) complex, K104 was synthesized as a chemotherpeutic. The cytotoxicity of K104 against various human cancer cell lines were evaluated by MTS assay in vitro. The IC50 values of K104 ranged 15.83-25.83
$\mu\textrm{M}$ , compared to CBCDA ranged 23.24-69.6$\mu\textrm{M}$ . Among several cancer cell lines, K104 showed more potent than CBCDA in colon cancer cell lines. (omitted) -
Lee, In-Ki;Yell, Shin-Chang;Bup, Sohn-Jin;Young, Jeong-Mi;Son-Miwon;Jun, Bae-Cheol;Soo, Byun-Jong;Kim, Dong-Sung;Kim, Soon-Hae 132.2
The biological effects of NADPH-dependent isocitrate dehydrogenase (IDPc) inhibitor, DA-11004, was investigated in obese diabetic (ob/ ob) mice. DA-11004, metformin, and oxalomalate were daily injected (ip) for 8 weeks and after completing an 8-week period of experiment, mice were sacrificed at 1 hr after the last drugs treatment to collect their blood, liver, and adipose tissues(epididymal and retroperitoneal fat). (omitted) -
Kim, H.D.;Park, J.H.;Lee, S.S.;H, Son-M.;Y, Kwak-W.;S, Yang-J.;I, Lim-J;Kim, S.H.;Kim, W.B. 133.1
Cathepsin K (CK) is a cysteine protease that plays a major and essential role in osteoclast-mediated degradation of collagen matrix of bone. Its tissue-limited distribution and pivotal contribution to bone resorption meet the requirements as the potential therapeutic target of the disease with excessive bone loss such as osteoporosis. In a search for potent CK inhibitors. we found OST-5440 that effectively inhibited bone resorption in vivo as well as in vitro. (omitted) -
2-Methylaminoethyl-4, 4'-dimethoxy-5, 5', 6.6 -dimethylenedioxybiphenyl-2'-carboxy-2-carboxylate (DDB-S), a synthetic compound derived from DDB, has been known to protect liver against carbon tetrachloride-, D-galactosamine-, thioacetamide-, and prednisolone-induced hepatic injury in experimental animals. The metabolism of this compound has been assessed in rats by using liquid chromatography/electrospray tandem mass spectrometry (LC/MS/MS) method. (omitted)
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Tempting to further understanding the biophysical mechanism of action of chlorhexidine, we examined effects of the antimicrobial agent(chlorhexidine digluconate) on rate of rotational mobility of liposomes of total lipids extracted from anaerobic bacterial outer membranes (Porphyromonas gingivalis outer membranes). (omitted)
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Seong, Min-Je;Song, Youn-Sook;Lee, Yoot-Mo;Jeon, Gye-Hyun;Shin, Im-Chul;Oh, Ki-Wan;Kim, Tae-Seong;Han, Soon-Young;Hong, Jin-Tae 134.2
A large number of chemical pollutants including phthalates, alkylphenolic compounds, organochlorine pesticides and bisphenol A have the ability to disrupt endocrine function in animals. and alter cognitive function. Because hormone mediated events playa important role in central nervous system development and functions. The speculations that the changes in cognitive function are mediated by the endocrine-like action of these chemicals. (omitted) -
We have previously reported three new oleanene-type glycosides and kudzusaponin
$A_3$ methyl ester and subproside II methyl ester from the roots of Echinosophora koreensis. Further study has now led to the isolation of three known oleanen-type glycosides. sophoraflavoside I, azukisaponin V, and kudzusaponin$SA_3$ as their methyl esters. The structures of theses compounds were characterized by spectroscopic and chemical methods. -
We studied the effect of methanol extract of Pachydictyon coriaceum (PC) on atopic allergic reaction. PC dose-dependently inhibited interleukin (IL)-8 and tumor necrosis factor (TNF)-
$\alpha$ secretion from the PMA- pius A23187- stimulated HMC-1. PC also dose-dependently inhibited the histamine and$\beta$ -hexosaminidase release from mast cells. PC had no cytotoxic effect. (omitted) -
Liriope platyphylla (LP) Wang et Tang has been used for tonic, anti-tussive and expectorant in Korea. In the current study, we found that buthanol fraction of Liriope platyphylla-conditioned media of C6 and primary astrocyte induced the neurite outgrowth of PC 12 cells, which effect was reversed by addition of NGF-antibody. We demonstrated that buthanol fraction of Liriope platyphylla increased the expression and secretion of NGF through RT-PCR and ELISA. (omitted)
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We studied the effect of methanol extract of Sargassum hemiphylum(SH) on atopic allergic reaction. SH dose-dependently inhibited interleukin (IL)-8 and tumor necrosis factor (TNF)-
$\alpha$ secretion from the PMA- plus A23187- stimulated HMC-1. SH also dose-dependently inhibited the histamine and$\beta$ -hexosaminidase release from mast cells. (omitted) -
Kim, Jin-Ho;Kim, Soo-Yeon;Lim, Yong;Park, Byeoung-Soo;Pyo, Hyeong-Bae;Yoo, Hwan-Soo;Yun, Yeo-Pyo 136.2
It was previously reported that luteolin, a flavone compound, displayed the potent anti-oxidant and anti-inflammatory effects, which have also been successful in reducing vascular smooth muscle cells(VSMCs) proliferation after arterial injury. Proliferation of VSMCs plays an important role in development of astherosclerosis. In this study, a possible anti-proliferative effect and its mechanism on rat aortic VSMCs by luteolin was investigated. (omitted) -
Myristicin, 1-allyl-3, 4-methylenedioxy-5-methoxybenzene, is a naturally occurring alkenylbenzene compound. It is found in nutmag, mace, parsley, carrot, black pepper, many natural oils and flavoring agents. The aim of this work was to identify the form(s) of human liver cytochrome P450 (P450) involved in the hepatic transformation of myristicin to its major metabolite, 5-allyl-1-methoxy-2, 3-dihydroxybenzene (M1). (omitted)
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The steam distillate obtained from sawdust of Thujopsis dolabrata var. hondai was fractionated by centrifugal thin-film evaporation. and then the fractions were investigated against antiplatelet activity using washed rabbit platelets in vitro. The biologically active constituent of T. dolabrata sawdust was isolated by silica gel column chromatography and HPLC and characterized as carvacrol by various spectral analysis (
$^{1}H$ ,$^{13}C$ -NMR and GC/MS studies). (omitted) -
$\beta$ -Eudesmol is one of various compounds derived from the bark of Magnolia obovata Thunberg, a medicinal plant. It has been shown that$\beta$ -eudesmol also markedly alleviated muscle fasciculation, tremor and convulsion induced by diisopropylfluorophosphate and prolonged the time to death in mice (Chiou et al., 1995). Actually, the extract of magnolia bark has been shown to have depressant actions on the cental nervous system (Watanabe et al., 1973). (omitted) -
Yin, Shou-Yu;Kim, Yu-Mi;Lee, Jae-Joon;Jin, Chun-Mei;Yang, You-Jong;Kang, Min-Hee;Lee, Myung-Koo 138.2
The inhibitory effects of (1R, 9S)- and (1S, 9R)-enantiomers of$\beta$ -hydrastine (BHS) on dopamine biosynthesis in PC12 cells were investigated. (1R, 9S)-BHS decreased the intracellular dopamine content with the$IC_{50}$ value of 14.3$\mu\textrm{M}$ at 24 h, but (1S, 9R)-BHS did not. In these conditions, (1R, 9S)-BHS inhibited TH activity mainly in a concentration-dependent manner(33% inhibition at 20$\mu\textrm{M}$ ) and decreased TH mRNA level. (omitted) -
Jin, Chun-Mei;Lee, Jae-Joon;Yin, Shou-Yu;Kim, Yu-Mi;Yang, You-Jong;Ryu, Si-Yong;Lee, Myung-Koo 139.1
The effects of liriodenine, an aporphine isoquinoline alkaloid, on dopamine biosynthesis and L-DOPA-induced neurotoxicity in PC12 cells were investigated. Treatment of PC12 cells with liriodenine at 10$\mu\textrm{M}$ showed 33.6% inhibition of dopamine content decreased at 3 h and reached a minimal level at 12 h after the exposure to liriodenine at 10$\mu\textrm{M}$ . (omitted) -
Tannin-rich fruit of Cornus officinalis Sieb. et Zucc has been used as an ingredient in several prescriptions of Oriental medicine. Cornis fructus was extracted by successive extraction. Cornis fructus extracts were investigated for antimicrobial and antioxidative activities. Antimicrobial effects used disk diffusion method. All extracts were examined against Streptococcus mutans. (omitted)
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The diterpene acid 1 was isolated from the roots of Anisotome lyallii(Apiaceae/Umbelliferae). The structure of the compound was elucidated as anisotomenoic acid 1 on the basis of spectroscopic method. This compound was evaluated against p388 murine leukaemia and B16/F10 melanoma cells.
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Sauchinone, a lignan isolated from Saururus chinensis (Saururaceae), is a diastereomeric lignan with cytoprotective and antioxidant activities in cultured hepatocytes. The effects of sauchinone on the iNOS, TNF-
$\alpha$ and COX-2 gene expression and on the activation of transcription factors, NF-$\kappa$ B, C/EBP, AP-1 and CREB were determined in Raw264.7 cells as part of the studies on its anti-inflammatory effects. (omitted) -
The inhibitory effect of 13(E)-Labd-13-ene-8
$\alpha$ 15-diol(1), isolated from the ethanol extract of Brachyglottis monroi, on the proliferation of human breast cancer MDA-MB231 cells was examined. Compound (1) at concentration as high as 16$\mu$ /$m\ell$ has inhibited the proliferation of MDA-MB231 and this cytotoxic effect was increased in a time and dose-dependent manners. (omitted) -
Subendothelial accumulation of foam cells plays a key role in the initiation of atherosclerosis. These foam cells accumulate in fatty streaks that evolve to more complex fibrofatty or atheromatous plaques. Oxidized LDL may also be involved in atherogenesis by inducing smooth muscle cell proliferation and smooth muscle foam cell generation. (omitted)
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The inverse relationship between dietary flavonoids consumption and cardiovascular diseases may be associated with the ability of flavonoids to attenuate LDL oxidation. Although flavonoids have been employed to prevent against LDL oxidation, their pro-oxidant effect also deserves an attention in respect to untoward property. (omitted)
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Excessive accumulation of beta-amyloid (A
$\beta$ ) peptides is one of the leading hypotheses to explain neurodegenerative processes in Alzheimer's disease (AD). It has been suggested that$A\beta$ toxicity is associated with increases in reactive oxygen species. whose overproduction may in turn initiate neurotoxic events. (omitted) -
We studied the effect of methanol extract of Carpopeltis affinis (CA) on atopic allergic reaction. CA dose-dependently inhibited interleukin (IL)-8 and tumor necrosis factor (TNF)-
$\alpha$ secretion from the PMA- plus A23187- stimulated HMC-1. CA also dose-dependently inhibited the histamine and$\beta$ -hexosaminidase release from mast cells. CA had no cytotoxic effect. (omitted) -
In this study. we investigated whether the cardioprotective effect shown by quercetin 3-O-
$\alpha$ -arabinofuranoside extracted from Lindera erythrocarpa against ROS-induced cell death in H9c2 cardiac myocytes. Cell death was induced by BSO, buthionine sulfoximine, which inhibits GSH level and subsequntly increase ROS level. Cell death was quntitatively determined by measuring lactate dehydrogenase (LDH) activity. (omitted) -
Joins (SKI 306X) is now clinically used for the treatment of osteoarthritis (OA). In previous reports, Joins a natural herbal product extracted from three herbs Clematis Radix. Trichosanthes Radix and Prunella Flos, was shown to have good analgesic and anti-inflammatory effects in several in vivo models. e.g., acetic acid-induced pain, carrageenan-induced paw edema and adjuvant-induced arthritis. (omitted)
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Several lines of recent evidences have shown that several pro-inflammatory genes or mediators, such as inducible nitric oxide synthase (iNOS), cyclooxygenase-2 and cytokines (e.g., tumor necrosis factor
$\alpha$ and interleukin-1$\beta$ ), are strongly expressed in the ischemic brain. Inflammation is now recognized as a significant contributing mechanism in cerebral ischemia because anti-inflammatory compounds or inhibitors of iNOS and cyclooxygenase-2 have been proven to reduce ischemic brain damage. (omitted) -
Koo, Hye-Jin;Song, Yun-Seon;Jin, Chang-Bae;Jung, Kyung-Ja;Lee, Sang-Hyun;Shin, Kuk-Hyun;Park, Eun-Hee 145.2
Gardenia jasminoides Ellis has been used in traditional medicine for the treatment of inflammation, jaundice, headache, fever and hypertension. The 70% ethanolic extract of gardenia fruit showed strong anti-angiogenic activity in the chick embryo chorioallantoic membrane (CAM) assay. Among hexane, ethyl acetate, n-butanol and aqueous fractions prepared from the 70% ethanolic extract, the n-butanol fraction was found to be most effective in the CAM assay. (omitted) -
Kim, Joo-Hyon;Lee, Hae-In;Jung, In-Ho;Jung, Ki-Won;Han, Chang-Kyun;Kwak, Wie-Jong;Cho, Yong-Baik;Joo, Hee-Jae 146.1
Joins (SKI 306X) is now clinically used for the treatment of osteoarthritis (OA). In previous reports, Joins, a natural herbal product extracted from three herbs Clematis Radix, Trichosanthes Radix and Prunella Flos, was shown to have good analgesic and anti-inflammatory effects and cartilage protective effects in several experimental models. In this study we characterized the effects of Joins on the gastric mucosa and compared to that of diclofenac. (omitted) -
Rhee, Hae-In;Kim, Joo-Hyon;Cho, Yong-Baik;Ryu, Keun-Ho;Han, Chang-Kyun;Yoo, Hun-Seung;Kim, Taek-Soo;Jung, In-Ho;Kwak, Wie-Jong 146.2
Lonicera japonica is widely distributed in Southeast Asia and has been traditionally used as an anti - inflammatory, diuretic, abscessic, antipyretic, and antidotic agent. Lonicera japonica was investigated for its anti-inflammatory and analgesic effects using several in vivo models. SKLJI was purified for i.v. injection from Lonicera japonica as a potent anti-inflammatory and analgesic fraction, after activity-guided fractionation study. (omitted) -
The present study was investigated the effect of berberine on the development of behavioral sensitization by morphine, methampethamine, and cocaine. Repeated administration of morphine (10 mg/kg), methampethamine (2 mg/kg), and cocaine (15 mg/kg) produced behavioral sensitization in mice. Pretreatment with berberine (2 mg/kg) did not inhibit methampethamine-and cocaine-induced behavioral sensitization. (omitted)
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Dongchunghacho is traditionally believed to be effective against various diseaseas. It includes many different genera such as Cordyceps, Paecilomyces, Torrubiella and Podonectria. The three fungus strains, Cordyceps militairs, Cordyceps scarabaeicola and Paecilomyces tenuipes were individually cultivated as supension cultures in potato dextrose broth. (omitted)
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The effects of methanolic extracts of Polygalae Radix (PR 100mg/kg) was tested to evaluate on the neuroprotective activity (92% p<0.001) on global cerebral schemia. Based on bioassays guided fractionation, butanol soluble fraction (BtOH 25mg/kg) had the neuroprotive effect (87% p<0.001) of global cerebral ischemia in rat. Oxygen free radical injury plays an important role in neuronal damage induced by brain ischemia and reperfusion. (omitted)
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The inhibitory effect of the lectins (KML-C) isolated from Korean mistletoe (KM; Viscum album coloratum), on tumor metastases produced by highly metastatic murine tumor cells, B 16-BL6 melanoma, colon 26-M3.1 carcinoma and L5178Y-ML25 lymphoma cells, was investigated in syngeneic mice. (omitted)
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Active ingredients, therapeutic and adverse effects of Aloe vera were comprehensively investigated. Aloe vera contains active components. including sugars, proteins, lipids, vitamins, minerals, phenolic compounds and other several compounds like phthalate esters, gibberellin, lectin-like substances, lignin, saponins, salicylic acid and uric acid. (omitted)
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Kang, Hye-Na;Oh, Ho-Jung;Kim, Soon-Nam;Hong, Choong-Man;Lee, Ki-Hong;Yoo, Si-Hyung;Shin, In-Soo;Choi, Seung-Eun;Lee, Seok-Ho 149.2
We have carried out a collaborative study to evaluate a candidate preparation of antithrombin III concentrate whether it is suitable to serve as a Korea National Biological Standard. Three National Control Laboratories and three manufacturers participated in this study. The potency of this candidate preparation was determined by using a heparin cofactor chromogenic method described in the Minimum Requirements for Biological Products and the European Phamacopoeia. (omitted) -
CYP3A4 is the most abundant human CYP and oxidizes a diversity of substrates. including various drugs. steroids. and carcinogens. A variety of metal ions are known to affect microsomal monooxygenase activities. Effects of a series of divalent metal ions on the CYP3A4-catalyzed reaction of reconstituted system containing purified CYP3A4. NADPH-P450 reductase (NPR), and cytochrome b5 (b5) were examined. (omitted)
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B cell translocation gene-1 (Btg-1), originally discovered from chromosomal translocation in chronic B-cell lymphocytic leukemia. belongs to the APRO family. Btg-1 exhibit antiproliferative function. being expressed during the
$G_{0}/G_{1}$ transition phase of cell cycle. Btg-1 is fully expressed in quiescent and differentiated cells. while the protein expression decreases as the cell progresses through the cell cycle. (omitted) -
Park, Hye-Ji;Kim, Su-Jin;Kim, Tae-Myung;Hong, Jin-Tae;Ha, Seang-Jong;Song, Jong-Yeol;Kim, Kee-Hyun 151.2
Bee venom (BV) has been utilized to relieve pain and to treat inflammatory diseases such as rheumatoid arthritis (RA). BV contains a variety of different peptides including melittin, apamin, adolapin and mast cell degranulating (MCD) peptide. In addition, it also contains enzyme (i.e. phospholipase A2), biologically active amines and non-peptide components. (omitted) -
This study was performed to investigate the effects of glycine on the development of tolerance to and physical dependence on morphine. Repeated adminstration of morphine developed tolerance and physical dependence. Glycine (100, 200 and 400 mg
$kg^{-1}$ i.p.) was administered intraperitoneally to mice for 7 days once a day 30 minutes prior to the morphine (10 mg$kg^{-1}$ s.c.). (omitted) -
We examined the effects of glycine on the morphine-induced hyperactivity, reverse tolerance and postsynaptic dopamine receptor supersensitivity in mice. A single administration of morphine (10 mg
$kg^{-1}$ s.c.) induced hyperactivity as measured in mice. The morphine-induced hyperactivity aws inhibited dose-dependently by the pretreatment with glycine(100, 200 and 400 mg$kg^{-1}$ i.p.). (omitted) -
This study was performed to investigate the effects of adenosine on the development of tolerance to and physical dependence on morphine. Repeated adminstration of morphine developed tolerance and physical dependence. Adenosine (1, 2 and 4 mg
$kg^{-1}$ i.p.) was administered intraperitoneally to mice for 7 days once a day 30 minutes prior to the morphine (10 mg$kg^{-1}$ s.c.). (omitted) -
Alternation and significance of calcium signalings through ryanodine receptor in neuronal cell deathHwang, In-Young;Lee, Sang-Min;Lee, Yoot-Mo;Kim, Su-Jin;Lee, Myung-Koo;Oh, Ki-Wan;Hong, Jin-Tae 153.2
Pathophysiological elevation of intracellular calcium concentration ([$Ca^{2+}$ ]$_i$ ) in the neuron has been considered as an important responsible factor in the neuronal cell damages. However, the mechanism of increase of [$Ca^{2+}$ ]$_i$ through ryanodine receptor (RyR), the relationship between [$Ca^{2+}$ ]$_i$ level and cell damages have not been fully demonstrated. (omitted) -
Hydroxyproline (HYP) is a post-translational product of proline hydroxylation catalyzed by an enzyme prolyl 4-hydroxylase which plays a crucial role in the synthesis of all collagens, because the 4-hydroxyproline residues are essential for the folding of the newly synthesized collagen polypeptide chains into triple-heical molecules. Considering the role of collagen and its significance in many clinically important diseases such as liver cirrhosis, a great deal of attention has been directed toward the development of an assay at cell-based system. (omitted)
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Lee, Jin-Soo;Whang, Yun-Ha;Ahn, Seok-Hoon;PanSoo;Jin, Sang-Mi;Yi, Sun-Shin;Jung, Young-Ho;Suh, Hong-Suk;Ryu, Jei-Man 154.2
Recently, we developed a new anti-osteoporotic agent, DW-1350, which not only inhibited osteoclast formation but also induced osteoblast differentiation through the in vitro randomized screening studies. We identified inhibitory activities of DW-1350 for each step of osteoclast differentiation, fusion and pit formation process in co-culture system with mouse bone marrow and primary osteoblasts. (omitted) -
Lee, Jin-Soo;Ku, Sae-Kwang;Jung, Da-Hee;Jin, Youn-Goo;Park, Jae-Hoon;Yang, Hee-Bok;Jung, Yong-Ho;Ryu, Jei-Man 155.1
In the present study, the effect of DW-1350, a newly synthesized anti-osteoporotic agent, was evaluated in ovariectomized Rat. Female SD Rat mice underwent bilateral ovariectomy for prevention study that test article was administered from 2 days after ovariectomy for 6 weeks, for therapeutic study it was conducted from 6 weeks after ovariectomy for three months. (omitted) -
The protective and antioxidant effect of Solanum lycopersicum extract in liver fibrosis induced ratsThe adducts of lipid peroxidation and related aldehydic end are mediators of chronic poisoning and affect the development of chronic liver damage leading to fibrosis and cirrhosis. Substances delayed or suppresed lipid peroxidation could have an antioxidant and protective effect in liver disease. In this study, it was attempted to find out above mentioned effect of Solanum lycopersicum investigated in CCl4 induce liver fibrosis model. (omitted)
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Ryu, Jei-Man;Seong, Seung-Kyoo;Kim, You-Eun;Shin, Dong-Hyuk;Jung, Yong-Ho;Shin, Byong-Chul;Park, Kyong-Bae;Lee, Jong-Du 156.1
166Ho, a$\beta$ -emitting radionuclide, was incorporated within polyurethane film for possible application for the therapy of skin cancers. The aim of this study was to investigate skin irritant after radiation with 166Ho patch in rabbits and to estimate the efficacy of this therapy for skin cancer patients. Six NZW rabbits were used for skin irritant in this study. The dorsal hair of rabbits was removed with an electric clipper and blade. (omitted) -
Ryu, Jei-Man;Seong, Seung-Kyoo;Bae, Eun-Jung;Song, Young-Jun;Jung, Yong-Ho;Kwak, Chul;Park, Mun-Soo;Lee, Sang-Eun;Shigematsu, Akiyo 156.2
166Ho-chitosan complex (HC) is a new radiopharmaceutical approved in Korea for liver cancer. In these studies, therapeutic effect against prostate cancer and biodistribution of HC were evaluated in animal models using the technique of intraprostatic administration. For evaluation of the therapeutic effect, noble rats with AIT orthotopic or subcutaneous prostate cancer were used. (omitted) -
Carbofuran(CF) is one of the most widely used carbamate pesticides in the world applied for insect and nematode control. Due to its widespread use in agriculture and households, contamination of food, water, and air has become serious, and consequently adverse health effects are inevitable in humans, animals, wildlife and fish, it has reported that CF alone or in combination with other carbamate insecticides influences the level of reproductive and metabolic hormones such as thyroxine and corticosterone, and results in impairment of endocrine, immune behavioral functions. (omitted)
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Cadmium is well known as a toxic metal and has insulin mimicking effects in rat adipose tissue. To investigate the effect of CdCl2 on glucose transport and its mechanism, this study was performed in 3T3-L1 adipocytes. 10 and 25mM of CdCl2 exposed to cells for 12 hours increased 2-deoxyglucose uptake to 2.2 and 2.8 fold, respectively. Nifedipine, a calcium channel blocker, inhibited the 2-deoxyglucose uptake stimulated by CdCl2. (omitted)
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This study deals with the radiation protection effect of the pretreatment of
$\beta$ -carotene and combination with selenium on the DNA damage in mice after whole body${\gamma}$ -irradiation. This was obtained the radioprotective effect by evaluation of DNA damage levels in mice spleen and blood after irradiation. Six-week-old ICR male mice were administrated with$\beta$ -carotene and combination with selenium orally once a day for 5 days and then irradiated with 8.0 Gy of$\gamma$ -ray at a dose rate of 1.0 Gy/min. (omitted) -
The aim of this study was to investigate the protective effects of selenium and its combination with
${\beta}$ -carotene treatments prior to whole-body irradiation in mice. This was obtained the radioprotective effect of selenium and its combination with${\beta}$ -carotene by evaluation of DNA damage levels in mice spleen and blood after irradiation. (omitted) -
Persistent organic pollutants (POPs) have spread throughout the global environment to threaten human health and damage ecosystems. with evidence of POPs contamination in wildlife, human blood. and breast milk documented worldwide. Breast milk is an ideal medium for assessing exposures to POPs. POPs enter humans largely as contaminants of dietary animal products, where they sequester in adipose tissue, serum, and breast milk and equilibrate at similar levels on a fat weight basis. (omitted)
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Hwang Chil (Dendropanax morbifera Lev.) belongs to Aralia elata group. This plant is only found in Korea and is considered to be along with ginseng. The physiological activities of it have been reported as having scavenging effect on oxygen free radicals and anti-carcinogenic effect. As most of the anti-oxidants were effective on protecting hepatotoxicity from alcohol, hard tissues restoring and skin whitening, the effectiveness of Hwang Chil extracts was screened. (omitted)
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NAD(P)H:quinone oxidoreductase (quinone reductase: QR: EC1.6.99.2), a cytosolic FAD-containing flavoprotein, form one of the important component of the phase II drug-metabolizing enzyme systems. It is found in all mammalian species tested and is expressed in many organs including the liver. QR catalyses two-electron reduction of qui nones to hydroquinones thereby suppresses the formation of superoxide anion radical. (omitted)
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Cho, Mi-Ra;Lee, Kyung-Sup;Lee, Jung-Jin;Jin, Yong-Ri;Son, Dong-Ju;Shin, Hwa-Sup;Yun, Yeo-Pyo 161.2
We have previously reported that green tea catechins(GTC) displayed anti-thrombotic activity, and that this might be due to anti-platelet rather than anti-coagulation effects. In the present study, we have compared the anti-platelet activity and mechanism of epigallocatechin gallate(EGCG) and epigaliocatechin(EGC), which are two major components of GTC. (omitted) -
Yoo, Jae-Myung;Choi, Heon-Kyo;Choi, Bo-Yun;Park, Jeong-Euy;Lee, Yong-Moon;Yun, Yeo-Pyo;Yoo, Hwan-Soo 162.1
The purpose of this study was to determine the possibility of sphingolipid as a diagnostic marker for Myocardiac Infarction(MI), atherosclerosis-related cardiovascular disease. Sphingolipids are known to playa role in the occurrence of atherosclerosis in human blood vessels. Platelet-poor plasma(PPP) and washed platelets were prepared from healthy volunteers and MI patients, and sphingolipids analyzed. (omitted) -
Fumonisins are specific inhibitors of ceramide synthase in sphingolipid metabolism. The objective of this study was to investigate whether the elevation of free sphingoid bases 1-phosphate (S1P) are related to the fumonisin exposure. Sprague Dawley rats were injected i.p. with 10mg/kg fumonisin B1 (FB1), and kidney, liver, heart, lung, brain and serum were collected for sphingolipid analysis. (omitted)
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Arsenic is a ubiquitous element that ranks 20th in abundance in the earth's crust, 14th in the sea water, and is a component of several hundred minerals. Arsenic and its compounds are mobile in the environment. Groundwater contamination by arsenic is a serious threat to mankind all over the world and it can also enter food chain. Humans are exposed to this toxic arsenic from air, food and water. (omitted)
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Several epidemiological studies suggested that arsenic exposure was strongly correlated with the development of cardiovascular disease such as hypertension. In order to examine whether arsenic affects vasomotor tone in blood vessels, we investigated the effect of arsenic on agonist-induced vasorelaxation using the isolated rat aortic rings in vitro organ bath system.Treatment with arsenite inhibited acetylcholine-induced relaxation of aortic rings in a concentration-dependent manner. (omitted)
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Diesel motors exhaust particulate material. which is known to be mutagenic, has caused heavy air pollution. PM 2.5 diesel exhaust of vehicle was collected using a high-volume sample equipped with a cascade impact. The crude extract was fractionated according to EPA recommended procedure into seven fractions by acid-base partitioning and silica gel column chromatography. (omitted)
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Chronic exposure of arsenic is well known to be the cause of cardiovascular disease such as hypertension. In order to investigate the effect of arsenic on blood vessels. we examined whether arsenic affected agonist-induced contraction of aortic rings in isolated organ bath system. Treatment with arsenite increased vasoconstriction induced by phenylephrine or serotonin in a concentration-dependent manner. (omitted)
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This research was designed to examine the presence of mutagenic/carcinogenic compounds in airborne pollutants in diesel particulate matter using an integrated biological approach. Respirable air borne particulate matter (PM2.5: <2.5mm) was collected from diesel engine exhaust using a high-volume sampler equipped with a cascade impactor. (omitted)
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Diesel exhaust is suspected to cause acute and chronic adverse effects on health. In recent. the effect of estrogenic endocrine disruptor in diesel particulate matter was little studied. Therefore, we examined the estrogenic activity of respirable diesel exhaust particulate matter derived from diesel engine motor. PM2.5 diesel exhaust of vehicle was collected using a high volume samples equipped with a cascade impactor. (omitted)
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We investigated the effects of bisphenol A (BPA), endocrine disruptor, on the mixed lymphocyte reaction and TNF-
$\alpha$ production of antigen presenting cells in mice. Cells from mouse (C57BL/6) bone marrow were cultured with GM-CSF for 8 days and mature dendritic cells (DCs) were prepared. These DCs proliferation in response to Balb/c splenocytes was measured at 72 h of culture with BPA by tritiated thymidine incorporation ([3H]TdR) and [3H]TdR incorporation was determined by scintilation counting. (omitted) -
The important biological activities of estrogen were reproduction and physiological processes in a number of tissues, including liver, bone, brain, blood vessels, adipose tissue and so on. The regulation of estrogen level is important a prevention of estrogen-related disease. Ginkgo biloba extracts (GSE) are extracted from leaves of the Ginkgo biloba tree. GSE contains 24% phytoestrogen, which are kaempferol, quercetin, and isorhamnetin. (omitted)
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Lee, Hyo-Min;Yoon, Eun-Kyung;Lee, Gun-Young;Kim, Hyun-Jung;Yang, Ji-Sun;Yang, Ki-Hwa;Choi, Kyung-Hee;Kim, Sung-Whan 167.1
The human exposure level of cadmium can be varied by environmental level of cadmium and individual life style. This study was conducted to estimate current exposure of cadmium using up-to date in Korea. The exposure estimates were intended to representative of the general adult group with 60kg. This study quantified human exposure level of cadmium through food, air and soil except water because domestic all data was not detected. (omitted) -
This study was performed to evaluate Quality of spring water in seoul. After the revision the guideline of water Quality control on July 2002, the ratio of non-passed samples of spring water increased evidently(2001, 24.5%
$\rightarrow$ 2002, 37.5%). So Citizens of Seoul have been worried about what makes the difference between two years. To find out the major reason of that rapid increasement, the experimental results of standard plate count and psychrotrophilic bacteria in seoul were used. (omitted) -
This report surveyed the trends of the fatalities related to the drug-toxicant (DT) and the drug abuse(DA), requested to analyze to the Central District Office of National Institute of Scientific Investigation for a year, 2002. The mortality related to DT in men was more common than that in the women. The most common age group of DT intoxication was 30's. (omitted)
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Hydrogen cyanide is one of the toxic agents with carbon monooxide in fire victims and is released by combustion of nitrogen-containing organic material such as plastic and wool. Until now there are few reports about blood cyanide concentrations in fatalities by fire in Korea. So in this study we examined blood cyanide concentration in 12 cases of fire fatalities. (omitted)
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Han, Eun-Young;Yang, Won-Kyung;Lee, Jae-Sin;Park, Yong-Hoon;Kim, Eun-Mi;Lim, Mi-Ae;Chung, Hee-Sun 169.1
This study was designed to compare the results and concentraions of methamphetamine (MA) and its metabolite amphetamine (AP) in head hair and hair collected from different parts of the body (axullae, pubis, and leg). Hair of subjects (N=15) suspected for MA abuse was simultaneously collected. (omitted) -
Quantitative Analysis of amphetamines in hair by EI-GC-MS using SIM mode with uncertainty estimationYang, Won-Kyung;Han, Eun-Young;Lee, Jae-Sin;Park, Yong-Hoon;Kim, Eun-Mi;Lim, Mi-Ae;Chung, Hee-Sun 169.2
A method using EI-GC-MS is described for the determination of amphetamines in hair. The method is applied to simultaneous quantify amphetamines (methamphetamine, amphetamine, MDMA and MDA). Drugs were extracted in 1 % HCl in methanol from hair. After derivertization with TFAA, the resulting drugs were separated on HP-5MS column during a 16 min program and identified by mass spectrometry with the SIM mode(EI-GC-MS). (omitted) -
Carisoprodol(CSP), commonly prescribed as a skeletal muscle relaxant, is increasingly abused among young people for a recreational purpose in Korea. CSP may induce hallucination if it were ingested with large amounts, futhermore a carisoprodol overdose is considered fatal. Recently, we encountered overdoses of carisoprodol in 6 suicide cases. (omitted)
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Baeck, Seung-Kyung;Kim, Dong-Woo;Kim, Sun-Chun;Park, Woo-Yong;Jin, Kwang-Ho;Chung, Young-Ho;Park, Yun-Shin;Seo, Joong-Seok 170.2
The most common cause of death in fires is the inhalation of noxious gases rather than thermal injury. Carbon monoxide is well-known toxic component in fire atmospheres. However, the importance of hydrogen cyanide(HCN) as a toxic agent in the fire related fatalities(FRF) is under discussion. HCN is known to be produced in fires involving by the pyrolysis of polyacrylonitril (PAN) and other nitrogen-containing polymer. (omitted) -
In some tissues 17b-estradiol (E2) is known to increase endothelial NOS expression. In the present study we examined the effects of E2 on estrogen receptors (ERa and b) and inducible nitric oxide synthase (iNOS) expression and analyzed the mechanisms in rat peritoneal macrophages. (omitted)
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Retinoids have been shown to be effective in suppressing tumor development in chemical carcinogens such as N-nitroso-N-methylurea (NMU) and N-nitroso-N-ethylurea (NEU) induced mammary tumors in various animals. However, retinoids-mediated chemopreventive process, linked to transcription factor NF-kappaB activation on chemoprevention has yet to be studied. (omitted)
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Park, Chang-Won;Kim, Kwang-Jin;Kim, Jae-Hee;Suh, Soo-Kyong;Kim, Jong-Won;Kim, Kyu-Bong;Park, Jung-Won;Hwang, Kwan-Ik;Seo, Kyung-Won 172.1
3-Monochloro-1 ,2-propanediol (3-MCPD) produced during the acid hydrolysis of vegetable proteins (ex. soybean products) is food-contaminant material detected in acid-hydrolysed soy, bread, water, et al. 3-MCPD is currently being a matter of concern to safety. The nephrotoxicity of 3-MCPD and 3-MCPD metabolites has been reported to result from accumulating of metabolites in kidney tubules and inhibiting of renal metabolism of glucose and lactate. (omitted) -
Naringenin, a phytoalexin found in grapefruit. has been reported to exhibit a wide range of pharmacological properties. The aim of the present study is to evaluate the protective effect of naringenin on hepatic fibrosis induced by dimethylnitrosamine (DMN) in rats. Fibrosis was induced by intraperitoneal injection of DMN. Naringenin was given orally at 20 mg/kg and 50 mg/kg daily for 4 weeks. (omitted)
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Park, Jae-Hyun;Lee, Jong-Kwon;Kim, Hyung-Soo;Chung, Seung-Tae;Eom, Jun-H;Kim, Kyung-A;Paik, Soon-Young;Oh, Hye-Young 173.1
The present study was conducted to determine the effects of bis-carboxyethyl germanium sesquioxide(Ge-132) and caffeic acid phenethyl ester(CAPE) on immune system in female BALB/c mice. The mice were orally exposed continuously to Ge-132 (0, 50, 100, or 200mg/kg), or CAPE (0, 5. 10, or 20mg/kg) for 14 days. Immunomodulatory activity was evaluated by assessment of body and organ weight, lymphocytes blastogenesis, (omitted) -
Kim, Soon-Sun;Rhee, Gyu-Seek;Lee, Rhee;Kwack, Seung-Jun;Lim, Kwon-Jo;Park, Chul-Hoon;Lee, Geun-Shik;Jeung, Eui-Bae;Kil, Kwang-Sup 173.2
Many pesticides possess hormonal activity and have been thus classified as endocrine disruptors. Bioallethrin is one of the pyrethroids. synthetic derivatives of naturally occurring pyrethrins. These pyrethroids including bioallethrin have been developed as insectides due to their high insecticidal potency and low mammalian toxicity. Currently, bioallethrin is used to eradicate pests and insects in Korea, providing potential for human exposure. (omitted) -
The protective effects of acteoside, a phenylethanoid glycoside, on cabon tetrachloride-induced hepatotoxicity and the possible mechanisms involved in this protection were investigated in mice. Pretreatment with acteoside prior to the administration of carbon tetrachloride significantly prevented the increased serum enzymatic activities of alanine and aspartate aminotransferase in a dose-dependent manner. (omitted)
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Herbal medicines are increasingly being utilized to treat a wide variety of disease processes. In this study, we assayed the preventive and therapeutic effects of aqueous extract from the roots of Platycodon grandilflorum. A DC, Changil (CK) in human microvessel endothelial cell-1 (HMEC-1) angiogenesis. CK inhibited cell migration and in the presence of CK proliferation of HMEC-1 was inhibited in a dose-dependent manner. (omitted)
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The protective effects of acteoside, a phenylethanoid glycoside, on carbon tetrachloride-induced hepatotoxicity and the possible mechanisms involved in this protection were investigated in mice. Pretreatment with acteoside prior to the administration of carbon tetrachloride significantly prevented the increased serum enzymatic activities of alanine and aspartate aminotransferase in a dose-dependent manner. (omitted)
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Lee, Kyung-Jin;Kim, Young-Sup;Ryu, Si-Yung;Chung, Young-Chul;Choi, Chul-Yung;Cho, Young-Soo;Jeong, Hye-Gwang 175.2
Herbal medicines are increasingly being utilized to treat a wide variety of disease processes. We previously reported that aqueous extract from the roots of Platycodon grandiflorum A. DC (Campanulaceae), Changkil (CK), had hepatoprotective effects against acetaminophen induced liver injury. In the present study, we assayed the preventive and therapeutic effects of CK on experimental hepatic fibrosis induced by dimethylnitrogamine or carbon tetrachloride in rats. (omitted) -
The protective effects on hepatic fibrosis of an aqueous extract from the roots of Platycodon grandiflorum A. DC (Campanulaceae), Changkil (CK), in hepatic stellate cell line, CFSC-2G. The increased deposition of extracellular matrix by hepatic stellate cells following liver injury in a process known as activation is considered a key mechanism for increased collagen content of liver during the development of liver fibrosis. (omitted)
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Herbal medicines are increasingly being utilized to treat a wide variety of disease processes. In this study, we assayed the preventive and therapeutic effects of aqueous extract from the roots of Platycodon grandilflorum A. DC, Changil (CK) on experimental metastasis induced by melanoma cell (816F10) in C56BL6 mice. The functional specificity of CK was investigated in tumor cell metastasis. (omitted)
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Yun, Hye-Jung;Kim, Youn-Jung;Kim, Eun-Young;Kim, Young-Soo;Kim, Mi-Kyung;Lee, Seung-Ho;Jung, Sang-Hun;Ryu, Jae-Chun 177.1
Sophoricoside was isolated as the inhibitor of IL -5 bioactivity from Sophora japonica (Leguminosae). It has been reported to have an anti-inflammatory effect on rat paw edema model. To develope as an anti-allergic drug, genotoxicity of sophoricoside was investigated in bacterial and mammalian cell system such as Ames bacterial test and mouse lymphoma tk gene assay (MOLY). (omitted) -
Pomegranate, a small tree originating in Orient, belongs to Punicaceae family. The seeds contain an oil of which about 80% is rare trans 18 carbon fatty acid (punicic acid), and have highest botanical concentration of a sex steroid, estrone. Pharmacological properties of pomegranate extract have been studied, with anti-microbial, anti-parasitic, anti-viral. and anti-cancer effects. (omitted)
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Lee, Jeong-Ho;Lee, Ki-Nam;Ryu, Hyeong-Won;Lim, Jin-A;Lee, In-A;Chun, Hyun-Ja;Baek, Seung-Hwa 178.1
This study was carried out to evaluate cytotoxic effects of Houttuynia cordata THUNB extracts on A549 (lung cancer), MDA-MB231 (breast cancer), SNU-C4 (colon cancer) and B16 (mouse melanoma) cell lines. We have determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazoliumbromide (MTT) assay. The 150$\mu$ g/$m\ell$ concentration of methanol extract (63.81 %) of Houttuynia cordata THUNB was shown significantly antitoxic activity on A549 cell lines. (omitted) -
Yun, Hye-Jung;Kim, Youn-Jung;Kim, Eun-Young;Kim, Young-Soo;Kim, Mi-Kyung;Lee, Seung-Ho;Jung, Sang-Hun;Ryu, Jae-Chun 178.2
To develope the novel anti-allergic drug, many sophoricoside derivatives were synthesized. Among these derivatives, JSH-II-3, JSH-Ⅵ-3, JSH-Ⅶ-3, and JSH-Ⅷ-3 were selected and subjected to high throughput toxicity screening (HTTS) because they revealed strong IL-5 inhibitory activity and limitation of Quantity. Mouse lymphoma thymidine kinase ($tk^{+/-}$ ) gene assay(MOLY) and single cell gel electrophoresis (Comet) assay in mammalian cells were used as HTTS tool in our laboratory. (omitted) -
CKD-712, named S-YS49 is a chiral compound derived from higenamine (one component of Aconite spp.) derivatives. To compare the cytotoxicity of CKD-712 between in the absence and in the presence of S9 metabolic activation system, we performed try pan blue dye exclusion assay in Chinese hamster lung (CHL) cell. In CHL cells, the cytotoxicity (
$IC_{50}$ ) of CKD-712 was 92.9${\m}g$ /$m\ell$ and 186.1${\m}g$ /$m\ell$ in the absence and presence of S9 metabolic activation, respectively. (omitted) -
The cytotoxic activity of 13(E)-Labd-13-ene-8
$\alpha$ , 15-diol(1), isolated from the ethanol extract of Brachyglottis monroi was evaluated against tumor cell lines such as P388, SNU-C4 MDA-MB231, B 16 melanoma and A549 in vitro. By mean of spectral analysis particularly by the aid of various two dimensional NMR experiments, 1H-NMR and 13C-NMR signals of (1) was completely assigned, and thus the structure of (1) was established unambiguously. (omitted) -
Solanum lyratum (Solanaceae) has been used as a traditional analgesic, antipyretic and hepatoprotective agents in Korea. In this study, we investigated the hepatoprotective effect of ethylacetate extract of Solanum lyratum (SL) on the dimethylnitrosamine (DMN)-induced liver damage in rats. Oral administration of SL (150, 300 mg/kg daily for 4 weeks) into the DMN-treated rats remarkably prevented the elevation of serum alanine transaminase, aspartate transaminase and alkaline phosphatase levels. (omitted)
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Proanthocyanidins, one of the major natural polyphenolic compounds of grape has been reported to exhibit a wide range of pharmacological properties. In this study, we investigated the hepatoprotective effect of proanthocyanidins on the dimethylnitrosamine (DMN)-induced liver damage in rats. Oral administration of proanthocyanidins (20, 50mg/kg daily for 4 weeks) into the DMN-treated rats remarkably prevented the elevation of serum alanine transaminase, aspartate transaminase and alkaline phosphatase, and bilirubin levels. (omitted)
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Kim, Ok-Hee;Jun, Hye-Seung;Park, Mi-Sun;Eom, Mi-Ok;Jee, Seung-Wan;Ryeom, Tai-Kyung;Kang, Ho-Il 180.2
Capsaicin (8-methyl-N-vanillyl-6-nonenamide), a pungent ingredient of hot chili peppers, has been reported to possess substantial anticarcinogenic and antimutagenic activities. In the present study. we investigated the effects of capsaicin on pulmonary metastasis of B 16-F10 murine melanoma cells. as well as its mechanism of action. Capsaicin (i.p.. 2.5mg/kg) suppressed the number of lung colonies (58%) in experimental lung metastasis assay. (omitted) -
Polyphenolic compounds have been reported to exhibit a wide range of pharmacological properties. In this study. we investigated the hepatoprotective effect of skin and seed of grape which contain abundant polyphenol compounds on dimethylnitrosamine(DMN)-induced liver damage in rats. Ingestion of skin and seed of grape (10% diet, daily for 4 weeks) into the DMN-treated rats remarkably prevented the elevation of serum alanine transaminase, aspartate transaminase and alkaline phosphatase, and bilirubin levels. (omitted)
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Jeon, Tae-Won;Hyun, Sun-Hee;Kim, Nam-Hee;Lee, Sang-Kyu;Kim, Chun-Hwa;Lee, Dong-Wook;Woo, Hee-Dong;Yang, Gi-Hyeok;Jung, Hyun-Ho 181.2
Single and 28-day repeated dose toxicity studies of botulinum toxin type A(BTA) were carried out in ICR mice and SD rats. respectively. In the single dose toxicity study. BTA was injected intraperitoneally to male and female mice at a single dose of 40, 59, 89, 133 and 200 ng/kg. All animals died from 59 ng/kg. Some clinical signs were observed in most of both sexes from 59 ng/kg, but no signs were seen in all animals at 40 ng/kg. (omitted) -
Occupational exposure to cadmium (Cd) can result in brain disorders and olfactory dysfunction is the most well-known symptom. Recently Cd has been shown to induce apoptosis by activating MAPKs in various cell types. However, intracellular signaling pathways of Cd-induced cytotoxicity in neuronal cells is not known well. Thus, in the present study, we studied role of JNK and its well-known downstream transcription factor, c-JUN, in Cd-induced neuronal cell death. (omitted)
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Recent industrial society has human widely exposed to PAHs that are comming from the incomplete combustion of organic material as widerspread environmetal contaminants. Biological activities of PAHs are not known although PAHs are considered as carcinogens. The mechanism of action of PAHs has been studied extensively, however it is not clear how PAHs turn on CYP1A1 in human breast cancer. (omitted)
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Joung, Ki-Eun;Kim, Ji-Sun;Song, Hye-Weon;Sheen, Yhun-Yhong;Hong, Seung-Kwon;Kang, Soon-Beom;Kim, Ho;Cho, Sung-Il 183.1
Endometriosis is classically defined as the growth of endometrial glands and stroma at extra-uterine sites. Although it is a common gynecological problem accompanied by chronic pelvic pain, infertility, and adhesion formation, the etiology of this disease is unknown. Endometriosis pathogenesis may involve endocrine and immune dysregulation since uterine endometrial growth is regulated by sex hormone in concert with bioactive mediators produced by uterine immune and endocrine cells. (omitted) -
Oh, Ji-Young;Lee, Su-Jung;Shin, Jae-Ho;Kim, Tae-Sung;Moon, Hyun-Ju;Kang, Il-Hyun;Kim, In-Young;Kim, An-Keun;Han, Soon-Young 183.2
Zinc is known to have an inhibitory effect on apoptosis and an antioxidative effect scavenging reactive oxygen species (ROS) under oxidative stress. We studied the influence of zinc on cadmium-induced apoptosis especially associated with ROS in MCF-7 human breast carcinoma cell line. For the determination of appropriate experimental concentration and time, we excecuted MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] assay and DNA fragmentation assay. (omitted) -
In this study, we investigated the effect of cadmium on genes expression related to zinc homeostasis in HT22 hippocampal neuron cell line by RT -PCR and western blotting technics. In the time-course effect, cadmium up-regulated the relative levels of MT -I and MT -II to~b-actin at 4 hr after treatment. These effects were consistent with MT -I/II protein contents by western blot analysis. But MT -III, a specific MT isoform in brain, was not affected by cadmium. (omitted)
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Hyun, Sun-Hee;Kim, Nam-Hee;Kim, Chun-Hwa;Lee, Sang-Kyu;Lee, Dong-Wook;Jeon, Tae-Won;Lee, Jae-Sung;Jeong, Tae-Cheon 185.2
Effects of diallyl sulfide (DAS), a component of garlic, on thioacetamide-induced hepatotoxicity were investigated in male ICR mice. When mice treated subcutaneously with 100, 200 and 400 mg/kg of DAS in corn oil for three consecutive days, the activity of cytochrome P450 (P450) 2E1-selective p-nitrophenol hydroxylase was dose-dependently suppressed. In addition, the activities of P450 2B-selective benzyloxyresorufin O-debenzylase and pentoxyresorufin O-depentylase were dose-dependently induced by the treatment with DAS. (omitted) -
Cho, Mi-Young;Jung, Ki-Kyung;Nam, Kyung-Tak;Kang, Ju-Hye;Kang, Seog-Youn;Chung, Hye-Joo;Kim, Ju-Il;Lee, Young-Don;Na, Han-Kwang 185.3
It is well-known that bisphenol A(BPA), an industrial raw material for polycarbonate and epoxy resins, shows estrogenic activity. Recent research from our laboratory has shown that SPA disrupts interaction between thyroid hormone and its receptor in a non-competitive manner, and alters the thyroid-hormone dependent expression of growth hormone(GH) and prolactin(PRL). (omitted) -
Certain polycyclic aromatic hydrocarbons (PAHs) have been reported to induce cytochrome P450 (P450) 1A1 and 1A2. In the present studies, the effects of six well-known PAHs on the activities of hepatic and pulmonary P450 enzymes were investigated in male ICR mice. When mice were treated intraperitoneally with 3, 10 and 30 mg/kg of individual PAHs for 3 consecutive days, the activities of ethoxyresorufin- and methoxyresorufin-O-dealkylases were significantly and (omitted)
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A sexual dimorphism in terbufos (S-t-butylthiomethyl-O,O-diethyl phosphorodithioate: TBF) toxicity was not reported and remains unclear. Previously. we reported that TBF treatment showed sexual dimorphic effects on acetylcholinesterase (AchE) activity. We further investigated that sexual dimorphism of TBF was affected to age and brain-regional selectivity, and whether ovary plays an important role in the effect. (omitted)
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Kim, Nam-Hee;Hyun, Sun-Hee;Kim, Chun-Hwa;Lee, Sang-Kyu;Lee, Dong-Wook;Jeon, Tae-Won;Lee, Jae-Sung;Lee, Eung-Seok;Chae, Whi-Gun 188.1
2-Bromopropane (2-BP) is a major component of the mixture of SPG-6AR and Solvent 5200 that is a substitute of chlorofluorocarbon. Many female workers exposed to 2-bromopropane in a Korean electronic company were found to have amenorrhea and male workers were diagnosed with oligospermia. In the present studies, immunotoxic effects of 2-BP and an analog, 1,2-dibromopropane (1 ,2-DBP), were investigated in female BALB/c mice. (omitted) -
Kim, Nam-Hee;Jeon, Tae-Won;Hyun, Sun-Hee;Kim, Chun-Hwa;Lee, Sang-Kyu;Lee, Dong-Wook;Jeong, Tae-Cheon 188.2
To develop cytochrome P450 (P450) modulators with low toxicity from natural products, we have evaluated more than 20 compounds in mouse and rat models. Among those, the effects of 1,8-cineole and diallyl sulfide (DAS) were most profound in modulating P450 expression. In this presentation, the effects of 1,8-cineole and diallyl sulfide (DAS) on P450 expression were introduced. (omitted) -
Transcript profiling is a particularly valuable tool in the field of steroid receptor biology, as these receptors are ligand-activated transcription factors and therefore exert their initial effects through altering gene expression in responsive cells. Also, an increased awareness of endocrine disrupting chemicals (EDCs) and their potential to affect wildlife and humans has produced a demand for practical screening methods to identify endocrine activity. (omitted)
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Methylmercury (MeHg), one of the heavy metal compounds. can cause severe damage to the central nervous system in humans. Many reports have shown that MeHg is poisonous to human body through contaminated foods and has released into the environment. Despite many studies on the pathogenesis of MeHg-induced central neuropathy, no useful mechanism of toxicity has been established so far. (omitted)
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Yun, Yoon-Mi;Young, Cho-Nam;Lee, Ji-Yun;Kim, Chang-Jong;Sohn, Uy-Dong;Lee, Moo-Yeol;Shin, Yong-Kyoo;Sim, Sang-Soo 190.1
It has been previously reported that silica dose-dependently caused the increase of histamine release and arachidonic acid release in RBL 2H3 cells. In this study. to investigate role of arachidonic acid in inflammatory response including histamine release and reactive oxygen species (ROS) generation. we observed effects of mellitin on histamine release and ROSgeneration in RBL 2H3 cells. (omitted) -
Production of prostaglandins involved in renal salt and water homeostasis is modulated by regulated expression of the inducible form of cyclooxygenase-2 (COX-2) at restricted sites in the rat kidney. COX-2 expression in the kidney is regulated by dietary salt intake, but the mechanism of its action is not fully understood. We have previously that high salt regulates COX-2 expression in rat kidney. (omitted)
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Germanium is present in all living plant and animal matter in micro-trace quantities. Clinical trials and use in private practices for more than a decade have demonstrated germanium's efficacy in treating a wide range of serious afflications. including cancer, arthritis and senile osteoporosis. To investigate anti-inflammatory activity of organic germanium, we measured the effect of organic germanium on histamine release, (omitted)
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This study was conducted to examine the effect of subchronic oral administration of aloesin on changes in the body weight and blood biochemistry in rats. Aloesin were given orally at a rate of 100 mg/kg every 12 hours for 15 days. The rats in the control group received isotonic saline. Thebody weight and food consumption were measured every 12hrs immediately prior to each treatment throughout the study period. (omitted)
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Lee, Sang-Hee;Koo, Jae-Yeon;Kim, Sang-Sung;Lee, Jung-Youn;Cho, Ha-Won;Kim, Byung-Moon;Oh, Uh-Taek 192.1
Histamine is found in most tissues of the body and activates polymodal nociceptors via unmyelinated afferent C-fibres. We have demonstrated that bradykinin. acting at B2 bradykinin receptors. excites sensory nerve endings by activating capsaicin receptors via production of 12-lipoxygenase metabolites of arachidonic acid in dorsal root ganglion. Histamine is known to the activator of phospholipase A2- arachidonic acid pathway via a G-protein- coupled H1 receptor. (omitted) -
Capsaicin, a pungent ingredient in chili pepper, is known to excite sensory neurons that mediate pain sensation. This effect of capsaicin is determined by unique receptors and the capsaicin receptor (transient receptor potential subfamily V, member 1 (TRPV1)) was cloned recently. TRPV1 contains six transmembrane domains and three ankyrin repeats at N-terminal. This characteristic architecture is common in other ion channel in TRPV families. (omitted)
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The present study was done to determine the effect of trolox C. a hydrophilic analogue of vitamin E, on hepatic injury, especially alteration in vasoregulatory gene expression during ischemia and reperfusion. Rats were subjected to 60 min of hepatic ischemia in vivo. Rats were treated intravenously with trolox C (2.5 mg/kg) or vehicle (PBS, pH 7.4), 5 min before reperfusion. (omitted)
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Effect of phenylpropanoids on Phospholipase A2 (PLA2) and phosphodiesterase (PDE) activities in the asthmatic lung tissue were studied in guinea pigs. Bronchial asthma were introduced by the challenge of aerosolized ovalbumin (OA) in the double-chambered plethysmograph at twenty one days after sensitization of OA in guinea pigs. Bronchoalveolar lavage fluids (BALF) were taken by brochalveolar lavage with HEPES buffer. (omitted)
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Lee, Jin-Hee;Lee, Ji-Yun;Kim, Youn-Joung;Kim, Tae-Doo;Yoon, Mi-Yun;Sim, Sang-Soo;Kim, Chang-Jong 194.1
Phenylpropanoids originating from vegetable kingdom have some biological activity. In this experiments, effect of phenylpropanoids on the histamine release from mast cells were studied in vitro. Rat peritoneal mast cells were isolated by the discontineous gradients of Percoll and their histamine release by stimulation of compound 48/80 and A23187 at a concentration of 6.0$\mu\textrm{g}$ /$m\ell$ were determined. (omitted) -
Phenylpropanoids(PP), C6-C3 compounds, are widely distributed in many plants. In this experiments, effect of PP on sheep red bood cells (sRBC)-induced delayed type hypersensitivity (DTH) were studied in ICR male mice. SRBC were challenged by i.p. injection at two weeks after sensitization of Lp. injection of sRBC. Five days after the challenge of antigen, paw edema induced 24 hours after the last challenge by DTH, respectively. (omitted)
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Many kinds of phenylpropanoids(PP), C6-C3 compounds, are widely distributed in many plants. In this experiments, effect of PP on sheep red bood cells (sRBC)-induced Arthus reaction (AR) were studied in ICR male mice. SRBC were challenged by i.p. injection two weeks after sensitization of Lp. injection of sRBC. Five days after the challenge of antigen, paw edema induced 3 hours after the last challenge by AR. (omitted)
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Cinnamic acid derivatives (CAD) originating from medicinal plants have some biological activity. In this study. effect of CAD on heterologous passive cutaneous anaphylaxis (PCA) were studied by the method of Levine and Vaz(1970). Anti-serum was prepared from OA-sensitized male Balb/c mouse at two weeks after the last challenge of ovalbumin (OA) and alumina gel, and these serum diluted with HEPES buffer by means of the heterologous PCA titer, i.e. the highest dilution inducing PCA in rats. (omitted)
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Inhibitory Action of Cinnamic Acid Derivatives on Reversed Cutaneous Anaphylasis and Hemolysin TiterCinnamic acid derivatives(CAD) originating from vegetable kingdom have some biological activity. Effect of CAD on reversed cutaneous anaphylaxis (RCA) and hemolysin (HY) titer were studied in rats. Experiments were carried out to determine RCA as the skin edema induced at 2 hours after injection of 0.05
$m\ell$ /site of anti-rat serum rabbit serum. Drugs were orally administered at one hour before antigen challenge. (omitted) -
Parkinson's disease (PO) is a widespread neurodegenerative disorder. Even though PD has been studied in many aspects, it is still unknown the molecular signaling mechanisms linking reactive oxygen species (ROS) and neuronal apoptosis in PD. A better understanding of cellular mechanisms that occur in Parkinson's disease is essential for development of new therapies. In this study we investigated the signaling molecules involved in neuronal apoptosis induced by 6-hydroxydopamine (6-OHDA) in human SK-N-SH neuroblastoma cells as a model cellular system. (omitted)
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Neuronal hyperexcitability followed by high level of intracellular calcium and oxidative stress play critical roles in neuronal cell death in stroke and neurotrauma. Hence, KR-31378, a novel benzopyran derivative was designed as a new therapeutic strategy for neuroprotection possessing both anti-oxidant and potassium channel modulating activities. In the present study, we tested for its neuroprotective efficacy against oxidative stress-induced cell death in primary cortical cultures and further investigated its neuroprotective mechanism. (omitted)
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Song, Youn-Sook;Park, Hye-Ji;Hwang, In-Young;Lee, Sun-Young;Yun, Yeo-Pyo;Lee, Myung-Koo;Oh, Ki-Wan;Hong, Jin-Tae 197.2
Activation of the apoptosis program by an increased production of beta-amyloid peptides (A${\beta}$ ) has been implicated in the neuronal cell death of Alzheimer's disease. Bcl-2 is a well demonstrated anti-apoptotic protein, however, the mechanism of anti-apoptotic action of Bcl-2 in A${\beta}$ -induced apoptosis of neuronal cells is not fully understood. (omitted) -
Ischemia-induced changes in protein expression may provide important insights into the mechanisms of cellular damage and their potential recovery. In the present study, to investigate protein patterns changed in ischemic condition, the cortical and striatal tissue samples from the permanent and transient ischemic rat brain obtained by middle cerebral occlusion were analysed by proteomic approchese using 20-PAGE and MALOI-MS. (omitted)
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Choline is an important membrane phospholipid constituent and a neurotransmitter precursor that is minimally synthesized in brain. The long-term maintenance of brain choline concentration is dependent on choline transport from plasma, which occurs via saturable transport system at the blood-brain barrier. In the present study, we examined to elucidate the characteristics of transport of cationic amines, especially choline which is one of cationic amines, to BBS using conditionally immortalized rat brain capillary endothelial cell line (TR-BBB) in vitro. (omitted)
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The purpose of this study is to examine whether an brain to blood efflux system for taurine is present on the blood-brain barrier (BBB) or not and this efflux transport system is regulated by CNS cell damage with oxidative stress agent such as diethyl maleate (DEM) or tumor necrosis factor-a (TNF-
${\alpha}$ ), by using the brain efflux index (BEI) method. The brain efflux index value is defined as the relative amount of test compound efflux from cerebrum compared with that of a reference compound, [$\^$ 14/C] carboxyinulin, which has limited BBB permeability. (omitted) -
Park, Ki-Sook;Lee, Sang-Min;Lee, Rhee-Da;Han, Soon-Young;Park, Kui-Lae;Yang, Ki-Hwa;Song, Yuen-Sook;Moon, Dong-Chuel;Song, Suk-Gil 200.2
The effect of 15-deoxy-PGJ$_2$ on the differentiation of embryonic midbrain cells into dopaminergic neuronal cells, and the relationship between cell differentiation with activation of PPAR-yand possible signal pathway were investigated, 15-Deoxy-PGJ$_2$ increased neurite extension, a typical characteristics of the differentiation of embryonic midbrain cells isolated from 12 day's rat embryos in a dose-dependent manner. (omitted) -
Microglial cell can act for phagocytosis against abnormal particles in brain, which means that beta-amyloid produced from APP(amyloid precursor protein) can be phagocytosed by microglia when released. In contrast. when senile plaque has already been formed in brain cortex and hippocamphal region, microglia can also accelerate the AD pathogenesis due to chronic inflammatory action, which lead to neuron cell cytotoxicity. (omitted)
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Rg3 is a derivative of triterpenoid dammarane, which originally extracted from Red Ginseng, which have been known to have neuroprotective, vasodilator, antioxidative, antimetastasis, and direct anticancer effects. These various backgrounds of Rg3 can provide an additional interest in respect to the “hematopoiesis” in bone marrow and spleen cells. We, therefore, have investigated what effects and correlates of Rg3 (e.g. suppression and side effects) are affected in relation with the bone marrow and spleen cells of mouse. (omitted)
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Calcineurin inhibitors, cyclosporine A (CsA) and tacrolimus (FK506), have been studied extensively regarding their effects on T lymphocytes, but their effects on dendritic cells (DC) are relatively unknown. DC can really capture Ag from dead and dying cells for presentation to MHC class I-restricted CTL. The main targets for the immunosuppressive calcinerin inhibitors, FK506 and CsA. have been considered to be activated T cells, but not antigen presenting cells (APCs). (omitted)
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Calcineurin inhibitors, cyclosporine A (CsA)and tacrolimus (FK506), have been studied extensively regarding their effects on T lymphocytes, but their effects on dendritic cells (DC) are relatively unknown. DC can really capture Ag from dead and dying cells for presentation to MHC class I-restricted CTL. The main targets for the immunosuppressive calcinerin inhibitors, FK506 and CsA, have been considered to be activated T cells, but not antigen presenting cells (APCs). (omitted)
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As medicinal knowledge developed. population system has been migrating into the aged society. These aged society evokes the social problem of senile diseases. One of these. Alzheimer's Disease (AD) has been an issue. and its causative.
${\beta}$ -amyloid(A${\beta}$ ) has also been a key target in drug development. In AD, microglial cell affects neuron cells in any way of positive and negative. (omitted) -
Azheimer's Disease (AD) known as senile dementia accounts for 50% of all dementia cases and is in growing status as population goes up. Generally. AD is a progressive neurodegenerative disease and includes much of senile plaque in cerebral hippocampus and cortex in patient's brain. For decades. AD theory is explained by amyloid cascade hypothesis. In process of the hypothesis, amyloid hypothesis forms fibrillar form beta-amyloid peptide (A
${\beta}$ peptide) and extraordinarily accumulates in brain tissue, and lastly senile plaque is formed, which pathologically affect the brain. (omitted) -
Microglial cell is a monocyte involved in the brain, which acts for a primary immune reaction and phagocytosis. Microglia has also been considered to have a great role in AD pathogenesis due to its intact inflammatory and phagocytic responses against foreign invaders. In the study, we tried to investigate the modulation of activation of microglia using Rg1, a class of ginsenoside from red ginseng. which are known to protect neuron cells. (omitted)
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Han, Shin-Ha;Yun, Yun-Ha;Song, Young-Cheon;Park, Eun-Jung;Choi, Sung-Sook;Ha, Nam-Joo;Kim, Kyung-Jae 205.1
Bifidobacterium spp. is nonpathogenic. Gram-positive and anaerobic bacteria, which inhabit the intestinal tract of humans and animals. Bifidobacterium spp. plays important roles in human health. However. the influence of exogenous factors on species composition of fecal bifidobacteria is still unclear. In this study, we wished to determine whether presentation of exogenous OVA (10$\mu\textrm{g}$ /$m\ell$ ) could be enhanced by the culture supernatant of ten Bifidobacterium spp. (omitted) -
Yun, Yun-Ha;Han, Shin-Ha;Son, Han-Shik;Lim, Hee-Jung;Song, Young-Cheon;Park, Eun-Jung;Kong, Hyun-Seok;Lee, Sook-Yeon;Ha, Nam-Joo 205.2
This experiment was designed to evaluate the immune responses after treatment of diabetes by using water extract of traditional herbal drugs on the splenocytes and peritoneal macrophages in vivo. We found two herbal materials of the hypoglycemic agents based on inhibitory activity of${\alpha}$ -glucosidase. These potential herbal drugs which remarkably inhibited${\alpha}$ -glucosidase in STZ-induced diabetic mices (STZ 150 mg/kg, i.p.) were Mori radicis Cortex(MRC, 2.32 mg/mouse) and Cudraniae radicis Cortex (CRC, 2.24mg/mouse). (omitted) -
The immunomodulator Ginsan has been found previously by us to stimulate the secretion of high levels of IL -1. IL -6 and TNF-alpha in irradiated mice. These cytokines are known to induce proliferation and differentiation of hematopoietic progenitor cells from the spleen and bone marrow and to protect mice from DNA-damaging agents. The present studies were evaluated as a cytoprotective agent against toxicity of the alkylating drugs. (omitted)
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The immunostimulatory and host resistance effects of the Platycodon grandiflorum A. DC, changkil (CK) and inulin (CKI) isolated from CK were investigated in rats. SD rat were exposed to CK or CKI by gavages for 7days and isolated peritoneal macrophages and splenocyte were used for these studies. CK and CKI significantly enhanced peritoneal macrophages activities such as ROS production and phargocytosis. (omitted)
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Ursodeoxycholic acid (UDCA) has been known commonly improving hyperbilirubinemia and excretion abnormality of bromsulphalein, which are appeared in the liver, and reducing the release of cholesterol from bile duct. In our study, UDCA was aimed to know if the agent can inhibit the pathogenesis of AD by suppressing the microglial activation when stimulated particularly by A
${\beta}$ peptide, which is known a major cause of AD. (omitted) -
cAMP acts as a second messenger in the functional responses of various cells to hormones, cytokines and other agents. In turn, this nucleotide also modulates the signal transduction processes regulated by a range of cytokines and growth factors. The intracellular level of cAMP is regulated by a G protein coupled adenylyl cyclase and degradation is mediated by the phosphodiesterases (PDEs), a superfamily of enzymes that catalyze the hydrolysis of cAMP. (omitted)
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Lee, Hae-Sook;Cho, Min-Chul;Lee, Kyung-Ae;Baek, Tae-Woong;Hong, Jin-Tae;Myung, Pyung-Keun;Choe, Yong-Kyung;Yoon, Do-Young 207.3
Peroxisome proliferator-activated receptor (PPAR), a member of the nuclear hormone receptor superfamily, is a transcription factor activated by specific natural or synthetic ligands. It is involved in various cellular processes including adipogenesis, inflammation, cell cycle progression and carcinogenesis. Here, we report the production and characterization of a PPARgamma subtype-specific monoclonal antibody P${\gamma}$ 48.34A, which was raised against full-length human PPARgamma protein. (omitted) -
In recent, growing aged people in coupled with the increased senile dementia, Alzheimer's disease, has been a social interests to be cleared out. Alzheimer Disease(AD), first reported by Alios Alzheimer (1864-1915) in 1907, is a neurodegenrative disease. Nothing exact cause of AD is available by now, but in clinical founding
${\beta}$ -amyloid peptide(A${\beta}$ ) and microtubule associated protein($\tau$ protein) is to involved in the disease, and the most important feature in AD is Known to induce chronic inflammation to neuron cell. (omitted) -
Ginsan. a new polysaccharide isolated from Panax ginseng, has been previously reported as a good immunomodulator. In this study, we investigated the protective effect of Ginsan against a lethal sepsis induced by Staphylococcus aureus infection. The survival rate of mice treated with Ginsan 24 h prior to S. aureus infection was 80% whereas PBS-treated mice showed 20% of survival in the same infection. (omitted)
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We have previously shown that 2, 3', 4, 5' -tetramethoxystilbene(TMS) from synthetic trans-stilbene analogues, is one of the most potently selective inhibitor of recombinant human cytochrome P450 1B1 in vitro. In the present studies. the effects of TMS on the expression of cytochrome P450 1B1 were investigated in human cancer cell lines such as MCF-7 and HL -60. TCDD-stimulated P450 1B1 protein and mRNA expression was significantly suppressed by TMS in a dose-dependent manner. (omitted)
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Nitric oxide (NO) and prostagladins(PGs) produced by inducible nitric oxide synthase(iNOS) and cyclooxygenase(COX-2) are known as inflammatory mediator. Modulation of these enzymes, induced by many stimuli(LPS, IFN-gamma, TNF-alpha, phorbol ester, etc), is a potent strategy as treatment of inflammatory diseases. Treatment of murine macrophage RAW 264.7 cell line with indole compound(IND-6) markedly reduced lipopolysacchride(LPS) stimulated NO production in a concentration-related manner. (omitted)
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In this study, we investigated the effect of inhibition of proliferation and antioxidant effect on B16F10 murine melanoma cell. Also, we examined by MTT(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay and intracellular reactive oxygen intermediate levels and the levels of catalase(CAT), superoxide dismutase (SOD), and glutathione peroxidase(GPX) an adaptive response of oxidative stress on B16F10 murine melanoma cell of pretreated with hydrogen peroxide. (omitted)
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Ju, Jung-Hun;Jung, Sang-Hun;Cho, Soo-Hyun;Dang, The-Hung;Lee, Jee-Hyun;Kim, Mi-Kyeong;Lee, Seung-Ho;Ryu, Jae-Chun;Min, Kyung-Rak 210.2
Eosinophilic inflammation is the main histological correlate of airway hyperresponsiveness and tissue injury in the pathogenesis of bronchial asthma. Interleukin (IL)-5 appears to be one of main proinflammatory mediators that induce eosinophilic inflammation. Allergic IL -5-deficient mice do not generate eosinophilia in the bone marrow, blood or lung in response to allergen provocation. (omitted) -
There are now increasing evidences that free radicals and reactive oxygen species are involved in a variety of pathological events. Flavonoids. a group of polypenolic compounds, are widespread in the human food supply. This study was carried out to investigate the antioxidant activity of these compounds. myriceitn and (+)-catechin on B 16Fl0. murine melanoma cell line in oxidative stress. Oxidative stress was induced by exposure to hydrogen peroxide. (omitted)
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Glycosaminolycans (GAGs). such as heparin and heparan sulfate, are highly charged molecules and are of great biological importance. Protein-GAGs interactions play prominent roles in cell-cell recognition and cell growth. Acharan sulfate (AS), isolated from the giant African snail Achatina fulica, is a novel member of glycosaminoglycan families. It showed antitumor activity by the inhibition of angiogenesis. (omitted)
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2-Hydroxycinnamaldehyde is an active compound isolated from the Stem Bark of Cinnamomum cassia, a traditional oriental medicinal herb, which has been shown to inhibit tumor cell proliferation. In this study, we investigated the effects of 2-hydroxycinnamaldehyde on the cytotoxicity. induction of apoptosis and the putative pathways of its actions in human promyelocytic leukemia cells (HL-60). (omitted)
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Primary cultured rat hepatocytes injured by carbon tetrachloride as a model to screen for hepatoprotective effect. Four flavonoid compounds showed anti-hepatotoxic effect by decrease GPT. LDH activity and MDA level. Also screen for hepatoprotective, anti-oxidative and anti-apoptosis effects of baicalin and baicalein on chang cell treated with t-BHP. Mesured radical detoxifying enzyme, GST and antioxidant enzyme SOD, Catalase activity, GSH level and Cellular glutathion peroxidase activity. (omitted)
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Polyphenolic compounds including flavonoids are wide spread in the plant kingdom, and interested recently because epidemiological studies have suggested correlations between the consumption of polyphenol-rich plant foods and the prevention of chronic diseases. Soy is a main source of isoflavonoids which are high dietary intake for the oriental population. In this study, anti-inflammatory action of sophoricoside, an isoflavone glycoside isolated from immature fruits of Sophora japonica (Leguminosae family), has been demonstrated. (omitted)
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Alpha-viniferin was isolated from Carex humilis (Cyperaceae), and showed anti-inflammatory effects on carrageenin or histamine-induced paw edema in mice. To understand mode of the anti-inflammatory action. effects of alpha-viniferin on cyclooxygenase (COX)-2, iNOS, oxygen radicals and proinflammatory cytokines have been analyzed. Alpha-viniferin showed selective inhibitory effect with an IC50 value of 5
$\mu\textrm{m}$ on COX-2 activity but showed weak inhibitory effect on the synthesis of COX-2 transcript which was identified by RT-PCR. (omitted) -
Three mistletoe lectins (ML -I, ML -IIU, ML -IIL) have been identified in Europe based on sugar specificities for galactose(Gal) and N-acetyl galactosamine(GalNAc). Korean mistletoe lectins have been known as mainly ML -II type. In previous results, we suggested that there are two lectins, 64 KDa and 60 KDa, in Korean mistletoe lectin (KML -C). (omitted)
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MeOH extract obtained from the Kochia scoparia (KS) was observed to inhibit tumor necrosis factor-alpha (TNF-alpha), prostaglandins (PGs) and nitric oxide(NO) production in a lipopolysaccharide (LPS)-stimulated murine macrophage cell line, RAW 264.7. These effects of MeOH-KS were based on modulation of iNOS and COX-2 level. Western blot analysis showed that MeOH-KS reduced the iNOS and COX-2 level in LPS activated macrophages, in a dose dependent manner without cNOS and COX-1 protein level. (omitted)
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Reactive oxygen species play an important role in aging. carcinogenesis, and certain neurological disorders of human beings in addition to the host-defensive mechanism of inflammatory response. Murine macrophages Raw264.7 released superoxide anions via NADPH oxidase complex and nitric oxide (NO) via iNOS synthase when the cells were stimulated with unopsonized zymosan binding to complement receptor. (omitted)
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We investigated the in vitro effect of Acteoside , phenylpropanoid glycosides. is a natural product isolated from …. on proliferation, differentiation and cell cycle regulation in human promyelocytic HL -60 leukemia cells. Acteoside significantly inhibited the proliferation of HL -60 cells, with IC50 of about 30
$\mu\textrm{g}$ /$m\ell$ . It was also found to be a potent inducer of differentiation in human leukemia derived HL-60 cells through the examination of differentiation markers. (omitted) -
Velutin and betulinic acid were isolated as a cytotoxic principle from the dichloromethane extract of Korean mistletoe (Viscum album var. coloratum) by repeated silicagel chromatography and recrystallization. In in vitro analysis of cytotoxic activity using NIH-3T3 cells, dichloromethane extract of Korean mistletoe was shown to be highly cytotoxic against tumor cells. And we obtained active compound (reffered to VD-2 and VD-6) from the dichloromethane extract. (omitted)
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Neuronal apoptosis may contribute to the pathological neuronal loss in certain disease states such as neurodegenerative diseases. Staurosporine (ST), a nonselective protein kinase inhibitor, has been shown to induce apoptosis in a variety of cells including nerve cell lines. In this study, we investigated the neuroprotective effect of sauchinone, which is a unique lignan from Sauchinone Chinensis, on ST-induced apoptosis in C6 rat glioma cells. (omitted)
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We previously reported that acharan sulfate from the African giant snail Achatina futica showed the anticoagulant activity in vitro, but it was much less than that of heparin. In present study, the anticoagulant activity of acharan sulfate was investigated in vivo. Intravenous administration of acharan sulfate prolonged the clotting time (APTT) in mice and rats in a dose-dependent manner. (omitted)
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In previous study, we investigated the mechanism of suppression of inducible nitric oxide synthase (iNOS) and cyclo-oxygenase-2 (COX-2) by ergolide, sesquiterpene lactone from Inula Britannica. In this study, the suppression of iNOS and COX-2 by ergolide might be attributed to selective inhibition of NF-
$\_$ K/B signaling pathways. Here, we investigated the suppressionmechanism of NF-$\_$ K/B signaling pathways by ergolide in TPA-stimulated HeLa cells. (omitted) -
In the type II system. there are two elongation enzymes in E. coli, FabB is well-known to its ability to elongate cis-3-decenoly-ACP (C10:1) in unsaturated fatty acid synthesis, whereas FabF is important for the thermal regulation of fatty acid composition by its ability to elongate palmitoleic acid to vaccenic acid. based on their genetic mutation anaylsis. Radiochemical enzyme assay was performed using myristoyl-ACP as a substrate, which is known for general substrate of FabB and FabF. (omitted)
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A novel lectin has been purified from the fruiting bodies of the mushroom, Fomitella fraxinea, which belongs to bracket fungi by a combination of ion-exchange chromatography on DEAE-cellulose and gel filtration chromatography on Sephacryl S-200 HR. The lectin, designated as FFrL, was a homotetrametric protein with a molecular weight of 50 kDa as demonstrated by SDS-PAGE (sodium dodecyl sulfate-polyacrylamide gel electrophoresis) and MALDI-TOF-MS(matrix assisted UV laser desorption/ionization time-of flight mass spectrometry). (omitted)
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Dietary organosulfur compounds have been shown to inhibit the proliferation of tumor cells. Synthetic sulfur-containing compounds including oltipraz exert chemopreventive and hepatoprotective effects. We previously showed that synthetic allylthiopyridazine derivatives designated as K compounds induced apoptosis in SK-Hep-1 hepatocarcinoma cells (Eur. J. Cancer: 37, 2104-10, 2001). (omitted)
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2-Hydroxymuconic semialdehyde dehydrogenase catalyzes the conversion of 2-hydroxymuconic semialdehyde (HMS) to an enol form of 4-oxalocrotonate which is a step in the catechol-meta cleavage pathway. A tomC gene encoding 2-HMS dehydrogenase of Burkholderia cepacia G4, a soil bacterium that can grow on toluene, cresol, phenol or tricholoro ethylene, is identified in between catechol 2,3-dioxygenase gene and HMS hydrolase gene, its sequence is analysed and the enzyme is characterised. (omitted)
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RNA polymerase II (pol II) is known to cycle between hyperphosphorylated and hypophosphorylated forms during transcription cycle. These extensive phosphorylation/dephosphorylation event occurs in the C-terminal domain (CTD) of the largest subunit of pol II which consists of a tandemly repeated heptapeptide motif with consensus of YSPTSPS. (omitted)
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Effect of lipids on the oxidative inactivation of paraoxonasel (PON1), a HDL -associated antioxidant protein, was investigated, based on the hydrolysis of phenyl acetate. First. various fatty acids were examined for the prevention against the inactivation of PON1 byascorbate/Cu2+ system, which caused a remarkable (
$\geq$ 90%) inactivation of PON1, accompanied by a partial loss of histidine residues. (omitted) -
This research was designed to investigate the effects of Bassica oleracea L. (BO) fractions on the membrane fluidity of the liposomal phospholipid membranes. The sample BO was extracted and fractionated to six different types. methanol(BOM), hexane(BOMH). ethylether(BOMEE), etylacetate(BOMEA), butanol(BOMB) and aqueous(BOMA) fractions. The fluidity of dipalmitoylphosphatidylcholine(DPPC) liposomal membranes incorporated with BO fraction was measured by means of high-sensitivity differential scanning calorimetry(DSC). (omitted)
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Zou, Yani;Kim, You-Jung;Kim, Ji-Young;Kang, Dae-Yoen;Kim, Nam-Deuk;Lee, Kyung-Hee;Chung, Hae-Young 221.2
Expressions of cellular adhesion molecules (CAMs) are closely related to the formation of early atherosclerosis, an age-dependent vascular disorder. However. previous research provided only limited and conflicted reports on age-related alterations of CAMs' expressions and even much less is known the modulation of CAMs by calorie restriction (CR), In this study, expression of vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), E-selectin, P-selectin and platelet/endothelial cell adhesion molecule-1 (PECAM-1) in aorta and kidney were investigated by western blot and immuno-histochemical stain utilizing ad libitum (AL) and CR rat. (omitted) -
Bae, Gyu-Un;Kwon, Hyoung-Keun;Kim, Gwan-Tae;Kim, Yong-Kee;Yoon, Jong-Woo;Cho, Eun-Jung;Lee, Hyang-Woo;Han, Jeung-Whan 222.1
The signal transduction pathway leading to the activation of the p70s6k plays an important role in the progression of cells from G0/G1 to S phase of the cell cycle but remains incompletely characterized. We investigated the role of the Rho family G protein Rac1 in H2O2-mediated p70s6k activation. Transient expression of a dominant negative mutants of the small GTP-binding proteins Rac1 (Rac1N17) and Cdc42(Cdc42N17) showed reduced levels of slower migration on Western blots of one-dimensional SDS-PAGE in p70s6k and ERK1/2 by PDFG stimulation. (omitted) -
Renal dipeptidase (RDPase, EC 3.4.13.19), an ectoenzyme of renal proximal tubules, is covalently bound to outer leaflet of lipid bilayer via glycosylphosphatidylinositol (GPI)-anchor. Chitin is a major component of the shells of crustacea such as crab, shrimp and crawfish. This study was conducted to examine the effect of chitosan on RDPase release from renal proximal tubules. Nitric oxide (NO), highly reactive free radical, inhibits the release of RDPase from porcine proximal tubules. (omitted)
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Many studies have identified the phosphatidylinositol 3-kinase (PI3K) as a key regulator for various cellular functions including cell survival, growth and motility. We have previously shown that H-ras, but not N-ras. induces invasiveness and motility in human breast epithelial cells (MCF10A), while both H-ras and N-ras induce transformed phenotype. In the present study, we wished to investigate the functional role of PI3K pathway in H-ra-induced invasive phenotype and motility of MCF10A cells. (omitted)
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Glial cell-derived neurotrophic factor (GDNF) is a potent neurotrophic factor that enhances survival of midbrain doparminergic neuron. GDNF and its receptors are widely distributed in brain and are believed to be involved in the control of neuron survival and differentiation. GDNF increased proliferation and migration of Hs683 human giloma and C6 rat giloma cells in a dose-dependent manner. (omitted)
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Recent studies have revealed that bacterial biofilm production by the gram-negative bacteria is regulated by the quorum sensing signaling molecules, AHLs (N-acyl homoserine lactones). This suggests that inhibiting the AHLs could enhance the effects of antibacterial agents. Halogenated furanones purified from the red algae Delisea pulchra have been known to decrease quorum sensing responses by competitive inhibition of the AHLs. (omitted)
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Ginsenoside, major components of ginseng have been reported to show various biological activities including an increase of cholesterol metabolism. stimulation of serum protein synthesis, immunomodulatory effects. To explain these pharmacological actions, it is thought that ginseng saponins should be metabolized by human intestinal bacteria after they are orally administered. (omitted)
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To evaluate the antiallergic activities of puerarin and daidzin from the rhizome of Pueraria lobata, in vitro and in vivo inhibitory activities of these compounds and their metabolite daidzein were measured. Daidzein exhibited potent inhibitory activity on the B-hexosaminidase release induced by DNP-HSA and potently inhibited the PCA reaction in mice. (omitted)
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The inhibitory effect of kakkalide isolated from Puerariae flos on ethanol-induced lethality and hepatic injury were investigated. Intraperitoneally treated Kakkalide was weakly reduced the mortality associated with administration of ethanol and did not reduce alcohol hepatotoxicity. However, orally administered kakkalide and intraperitoneally administered irisolidone significantly reduced serum ALT and AST activities on liver-injured mice by ethanol. (omitted)
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Pancreatic lipase-inhibitory activity of the rhizome of Alpinia officinarum (AO) and its antihyperlipidemic activity were measured. When water extract of AO was stepwise fractionated with organic solvents, ethylacetate fraction exhibited the most potent inhibition. From it, Diarylheptanoid was isolated as an inhibitor of pancreatic lipase and we investigated its in vitro inhibitory effect of lipase activity and in vivo antihyperlipidemic effect. (omitted)
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The FimH subunit of type 1-fimbriated Escherichia coli has been determined as a major cause of urinary tract infection. To produce a possible vaccine antigen against urinary tract infection, the fimH gene was genetically linked to the Itxa2b gene, which was then cloned into the pMAL -p2E expression vector. The chimaeric construction of pMALfimH/Itxa2b was transformed into Escherichia coli TB1 and its N-terminal amino acid sequence was analyzed. (omitted)
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Lactic acid bacteria have been considered as the most beneficial probiotic organisms contributing to inhibition of harmful and putrefactive intestinal bacteria. Among them, Bifidobacterium spp. has been considered as one of the most beneficial probiotic organism that can improve the health of humans, since it is one of the major bacteria flora in human intestine. However, the harmful enzyme-inhibitory activity of lactic acid bacteria of Kimchi, which is a representative Korean fermented food has not been evaluated. (omitted)
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To assess the effect of chitosan complex with metal ion on various pathogenic bacteria, the antibacterial activities were investigated. Arsenic, bismuth, calcium, iodine, iron, mercury, platinum, and silver were used as a metal ion. Staphylococcus aureus. Streptococcus mutans, Helicobacter pylori, Propionibacterium acnes and human saliva were examined. It was demonstrated that metal ions associated chitosan showed aggregation activities on various pathogens.
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Jeong, Hye-Yoon;Jang, Seung-Jae;Lee, Song-Deuk;Min, Chung-Shik;Lee, So-Yeon;Lee, Kyung-Hee;Lee, Jung-Eun;Lee, Min-Seok;Lee, Kyung-Won 227.2
In the situation of high bacterial resistance to antibiotics in Korea, to assess diffusion of methicillin-resistant Staphylococcus aureus (MRSA) and levels of bacterial resistance to antibiotics in community, we monitored antibiotic resistance of S. aureus isolates from healthy volunteers of community. (omitted) -
Kim, Yun-Wha;Jeon, Soo-Jin;Kim, Ki-Sung;Han, Young-Soo;Song, Jie-Young;Park, Chang-Seo;Jung, In-Sung;Hong, Sung-Hee;Yun, Yeon-Sook 228.1
Sphingolipid metabolites have been implicated as an important component of cell signalling, such as cell proliferation, differentiation and apoptosis. But the roles of phytoceramide and its deraivatives are very poorly understood. even though they are abundant in plants, yeasts and animals including humans. We investigated the effects of N-acetyl-C2-phytosphingosine(NAPS) and the analogue of N.N-dimethylsphingosine(DMS), N,N-dimethylphytosphytosphingosine(DMPS), on cell growth inhibition and apoptosis. (omitted) -
Estrogen Receptor is a ligand-activated transcription factor. The concentration of the receptor is a major component that regulates expression of estrogen-responsive genes. We have studied mechanism of estrogen receptor alpha (ER
${\alpha}$ ) downregulation by HIF-1 using HIF-1${\alpha}$ /VP16 constructs. ER${\alpha}$ is known to be downregulated under hypoxic condition. Transcriptional response under hypoxia is mediated through Hypoxia-inducible factor-1 (HIF-1), a transcription factor that is usullaly degraded but stabilized under hypoxia. (omitted) -
Park, Sang-Eun;Yee, Su-Bog;Choi, Hye-Joung;Chung, Sang-Woon;Park, Hwa-Sun;Yoo, Young-Hyun;Kim, Nam-Deuk 229.1
The anti proliferative effects of bile acids and their derivatives on HT -29 human colon cancer cells were investigated. Ursodeoxycholic acid (UDCA) and its synthetic derivatives, HS-1030 and HS-1183, and chenodeoxycholic acid (CDCA) and its synthetic derivatives, HS-1199 and HS-1200 were employed for this study. General evaluations focusing on cell cycle were conducted in HT -29 human colon adenocarcinoma cell line (p53 mutant type). (omitted) -
Chung, Sang-Woon;Yee, Su-Bog;Choi, Hye-Joung;Park, Sang-Eun;Jung, Kyung-Jin;Kim, Dae-Hyun;Chung, Hae-Young;Kim, Nam-Deuk 229.2
Among the aldehydes derived from lipid peroxidation, 4-hydroxynonenal (HNE) that can be produced from arachidonic acids. linoleic acids, or their hydroperoxides in relatively large amounts in response to oxidative insult. Therefore, HNE might be an important mediator of Oxidative stress-induced apoptosis. To study the hypothesis that HNE may induce apoptosis, we estimated cytotoxicity of HNE on YPEN-1 rat prostatic endothelial cells. (omitted) -
Choi, Hye-Joung;Yee, Su-Bog;Chung, Sang-Woon;Park, Sang-Eun;Choi, Yung-Hyun;Jung, Jee-Hyung;Kim, Nam-Deuk 230.1
The marine sponge of the genus Petrosia sp. is known to contain unique metabolites such as furanoterpenoids. These furanoterpenoids have been reported to possess various bioactivities. We have shown previously that ircinin-1 induced cell cycle arrest and apoptosis in SK-MEL-2 human skin cancer cells dose- and time-dependently. In this study. we demonstrated that ircinin-1-induced apoptosis is a accompanied by cleavage of poly(ADP-ribose) polymerase protein and PLC-${\gamma}$ 1 degradation and release of cytochrome c from mitochondria to cytosol. (omitted) -
The seaweed, as source of bio-active substances as well as food, has received much attention in recent years. This study was carried out to determine the cytotoxic and chemopreventive effects of Porphyra tenera (PT) and Enteromorpha linza (EL). The PT and EL extracts from methanol were fractionated to five different types, which are hexane, ethylether, ethylacetate, butanol and water. (omitted)
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Ultraviolet (UV) irradiation is well known to cause human skin aging and skin cancer through activation of matrix metalloproteinases (MMPs) which are responsible for the degradation of collagen, an extracellular matrix component. However, the molecular mechanisms of UV-induced MMP expression are yet to be defined. In this study, we investigated signaling molecules involved in UV-induced MMP expression in HaCaT human keratinocytes. (omitted)
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The efficient EPO (Erythropoietin) expression system in Chinese Hamster Ovary (CHO) cells was devised through the removal of ammonium ion accumulated in the media by introducing urea cycle enzymes. Previously, we developed C05 cell by transfecting the carbamoly phosphate synthase (CPS) and ornithine transcarbamoylase (OTC) into the EPO expressing CHO cell, IBE. (omitted)
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Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics and some active compounds such as FR 173657, LF 16-0687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed to synthesize the analogues of FR173657 with two to three amide bonds and lipophilic ring system in each molecule. (omitted)
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Many neurodegenerative disorders such as stroke, Alzheimer's disease, and Parkinson's disease have been known to be associated with an excessive generation of reactive oxygen species (ROS) and oxidative stress. Therefore, the antioxidants have recently received much attention as therapeutic agent for the treatment of neurodegenerative disease. (omitted)
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Cho, Soo-Hyun;Yang, Hyun-Mo;The, Hung-Dang;Ju, Jung-Hun;Kim, Mi-Kyung;Lee, Seung-Ho;Ryu, Jae-Chun;Kim, Young-Soo;Jung, Sang-Hun 233.1
Interleukin (IL)-5 appears to be one of the main proinflammatory mediators among a growing number of cytokines and chemokines that induce eosinophilic inflammation. Sophoricoside and their analogs isolated from Sophora japonica show relatively potent inhibitory activity of interleukin (IL)-5 as a small molecule. Initial attempt to identify the structural requirement of this isoflavonone led to find new chalcones to exhibit the inhibitory activity of IL -5. (omitted) -
Diosgenin(25(R)-spirost-5-en-3
${\beta}$ -ol) is the steroid saponin, was isolated from Mexican yam(Oioscorea). Estrogenic, progesterogenic and anti-inflammatory effects of diosgenin has been hypothesized due to its structural similarity to estrogen, progesterone precursors. And diosgenin had been reported to lower serum cholesterol in chicken and rabbits fed cholesterol and to decrease liver cholesterol in cholesterol-fed rats. (omitted) -
The, Hung-Dang;Lee, Jee-Hyun;Cho, Soo-Hyun;Hong, Chang-Yong;Jeong, Shin-Wu;Jeon, Ki-Wan;Lee, Sung-Bae;Choi, Whan-Geun;Jung, Sang-Hun 233.3
Novel arylsulfonylimidazolidinones were previously demonstrated to have broad and highly potent cytotoxicities against a wide range of cancer cell line. Among them 4-phenyl-l N-(p-aminobenzoyl)indoline-5-sulfonyl imidazolidinone (PA) was proved to have good pharmacological profile. Recently modification of indoline moiety of PA led us to find new analogs which show better pharmacological profiles compared to PA. (omitted) -
Spicatoside A and spicatoside B were isolated from Liriopis tuber. Spicatoside A has anticancer activity and it is composed of 1
${\beta}$ -hydroxy diosgenin and trisaccharides. Spicatoside B has the preventive effect of diabetes mellitus and also has 1${\beta}$ -hydroxy derivatives, which is clevaged the ether linkage of F ring of diosgenin. Therefore, selective synthesis of 1${\beta}$ -hydroxydiosgenin is required. (omitted) -
Development of new tissue factor (TF) inhibitor is still needed for improved compositions having anticoagulant activity and which can be administed orally or non-intravenously at low doses. Our studies for the development of new TF inhibitors uncovered that aminoalcohols with C-18 alkenyl group, 9-octadecenyl- or 9,12-octadecadienyl groups exhibits in vitro nanomolar level activities. (omitted)
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The abundance of carbohydrates in nature with diverse roles in biological systems makes them a subject of considerable interest. They exhibit biological effects. ranging from cellular regulation to the selective inhibition of enzymes with key roles in living organisms. A wide range of carbocyclic polyhydroxyls has significant therapeutic effects, examples of which include cyclohexane hexitols, such as inositols, and pseudo-sugars, such as cyclophellitol and valienamine. (omitted)
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To decipher the structure-activity relationships of flavones for the inhibition of cyclooxygenase-2 catalyzed prostaglandin production, we synthesized 7-methxoyflavones, 7-hydroxyflavones, 5-methxoyflavones, 5-hydroxyflavones and flavones without any phenol group on A ring. Methoxyflavones were prepared from 2.6- and 2,4-dihydroxyacetophenones in 3 steps. Most of the methxoyflavones were converted to the corresponding hydroxyflavones by the reaction with BBr3 in good yields. (omitted)
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S-adenosyl-L-homocysteine(AdoHcy) is the product of all biological methylation in which S-adenosyl-L-methionine (AdoMet) is utilized as a methyl donor and is reversibly hydrolyzed to L-homocysteine and adenosine by AdoHcy hydrolase physiologically. Inhibition of this enzyme results in intracelluar accumulation of AdoHcy leading to a feedback inhibition of AdoMet-dependent methylation reactions which are essential for viral replication. (omitted)
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Bromofluoroacetophenone derivatives which produce fluorine substituted phenyl radicals that cleave DNA upon excitation were investigated as a novel photonuclease. Pyrrolecarboxamide-conjugated bromofluoroacetophenones: 4'-bromo-2'-fluoroacetophenone and 2' -bromo-4'-fluoroacetophenone were synthesized and their DNA cleaving activities and sequence selectivities were determined. (omitted)
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Several studies of terbenzimidazoles and bibenzimidazoles suggested that benzimidazoles, especially 5-nitro-2-(para-methoxyphenyl)benzimidazole. possess topoisomerase I inhibition activities. In order to find out the structure activity relationship of 5-nitro-2-phenyl-benzimidazoles. eight derivatives that are substituted at the para position of 2-phenyl moiety were selected, synthesized & evaluated considering their electronic or lipophilic parameters. (omitted)
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(2S 3R. 4E) 5-Aryl-4-pentene-1,3-diol-2-aminoueras had been synthesized for their cytotoxic activity. Pinene was oxidized with KMnO4 to give 2-hydroxy-3-pinanone. which treated with ethyl glycinate to yield iminoglycinate and then reacted with aldehyde derivatives and titanium enolate to afford 3-hydroxy aldol compounds. (omitted)
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A pathway for synthesis of N-methylspiro [1,2,3,4-tetrahydro-naphthalene-1,2'- pyrrolidine] was developed. Formation of the imine compound from
${\alpha}$ -tetralone and methylamine using titanium tetrachloride followed by ddition of allylmagnesium bromide gave (1-allyl-1,2,3,4-tetrahydro-naphthalen-1-yl)methylamine. (omitted) -
Carbonucleosides has extensively been studied as a promising anti-viral agents having chemical and metabolical stability. As yet there are no rules relating the structures of carbocyclic nucleosides to their therapeutic activity. although trends among certain kinds of structure have been tentatively put forward. In our research program for discovery of anti-viral drugs, the novel cyclobutyl nucleosides can be expected to be potential antiviral drugs as analogues of cyclobut-A, anti-HBV agent. (omitted)
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Tissue Factor (TF), a principal initiator of the veterbrate coagulation cascade is known to to induced in endothelial cells, monocytes and macrophages by inflammetry stimuli and in many pathological conditions. Through our synthetic efforts to develop new TF inhibitors, seventeen N-C-18 alkenyl group (9-octadecenyl or 9,12-octadecadienyl) substituted aminoalcohols (2-aminoethanol, 1-amino-2-propanol and 3-amino-1-propanol) were prepared and their in vitro TF inhibitory activities were examined. (omitted)
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An, Soo-Hyun;Oh, Chang-Hyun;Lee, Joo-Shin;Lee, Soo-Chul;Choi, Jung-Hun;Baik, Dae-Jin;Cho, Jung-Hyuck 238.2
The synthesis of a new series of 1${\beta}$ -methylcarbapenems having the substituted aminoethyl-carbamoylpyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituent on the pyrrolidine ring was investigated. In particular. the compound 11 g having piperazinyl urea moiety showed the most potent antibacterial activity. -
Among 4'-substituted nucleosides. Nucleocidin. 4'-azido thymidine (ADRT), 4'-fluorinated carbocyclic nucleoside. and 3'-fluoro oxetanosin analogue have demonstrated a variety of biological activities. Since the cyclopentane ring of carbocyclic nucleosides can emulate the furanose moiety. a number of these compounds exhibit interesting biological activity, particularly in the areas of antiviral and anticancer chemotherapy. (omitted)
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Suh, Young-Ger;Lee, Yong-Sil;Lee, Bo-Young;Min, Kyung-Hoon;Kim, Jin-Kwan;Seung, Ho-Sun;Park, Young-Ho 239.1
The vanilloid receptor VR has attracted great interest as a sensory transducer for capsaicin. protons, and heat. and as a therapeutic target. On the basis of the previous studies on vanilloid agonists and antagonists. we have looked for non-vanilloid VR antagonists by developing ideal vanilloid equivalents, which might provide the perfect analgesic effects without the side effects caused by vanilloid receptor agonists. (omitted) -
Studies on the Regioselective and Diastereoselective Amination using Chlorosulfonyl Isocyanate (CSI)We have recently described the novel synthetic method for N-protected amines from various ethers using chlorosulfonyl isocyanate(CSI) and found that the mechanism of our CSI reaction is a competitive reaction of SN1 and SNi mechanism according to the stability of carbocation intermediate. Forthermore. we developed the regioselective and diastereoselective one-pot synthetic method for 1,2-amino alcohol, through the reaction of di-and tribenzyl thers with CSI, and invetigated its mechanism. (omitted)
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Kwon, Soon-Kyoung;Park, Hae-Sun;Choi, Hee-Jeon;Park, Myung-Sook;Yoon, Myung-Sun;Kim, Nan-Young;Shin, Hae-Soon 240.1
Nonsteriodal antiinflammatory drugs(NSAIDs) are widely used to treat pain. fever, and inflammatory conditions including osteoarthritis. However, gastrointestinal (GI) and renal toxicity were related to common NSAIDs limits their usefulness because NSAIDs inhibit not only COX-2 associated with anti-inflammatory activity. but also COX-1 accompanied with side effects in the stomach and kidney. (omitted) -
A strategy for synthesis of the furan-fused tetracyclic core of xestoquinone and halenaquinone was explored through a model study. Methyl 8-oxo-4-methyl-4-phenyl-2,7-nonadiynoate was prepared from hydratroponitrile and 3-butyn-1-ol as starting materials. The intramolecular cycloaddition of this intermediate as a key step will be involved.
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Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand, neplanocin A and aristeromycin are the representative of the carbocyclic nucleosides and have been recognized as potent inhibitors of S-adenosylhomocysteine hydrolase. Based on these findings. it was of great interest to design apio analogues of neplanocin A and aristeromycin. (omitted)
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We report the synthesis of key intermediates for the development novel flavonoid derivatives with potential antiinflammatory activity and propose a mechanism of the one-pot reaction. The various amines (1) for this work were commercially available. Secondary amines (2) were formed by nucleophilic attraction using ethyl benzoylacetate. The C-N bond formation proceeded at refluxing in toluene with catalytic amount of p-toluenesulfonic acid and a removal of water was important in this reaction. (omitted)
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Kim, Hee-Doo;Yoon, Jung-Wha;Choi, Hye-Young;Lee, Hyun-Joo;Ryu, Chong-Hyun;Park, Young-Ho;Suh, Young-Ger;Oh, Uh-Taek;Park, Hyeung-Guen 241.3
By acting on vanilloid receptor(VR1). capsaicin excites and then desensitizes a subset of primary neurons involved in nociception, neurogenic inflammation, and a variety of local regulatory functions. Due to this unique biological activity, VR1 is at present one of the most attractive targets for the treatment of pain. However, despite the concentrated effort on agonists, they have been exposed to the side effects such as pungency and/or hypothermia responses. (omitted) -
Woo, Seong-Ju;Lee, Hae-Sung;Cheong, Min-Young;Ahn, Kwang-Hyun;Park, Ki-Seok;Koo, Chang-Hui 242.1
The nucleoside analogue, L-FMUS was synthesized from L-FMAU which has been shown to have significant antiviral activity against hepatitis B virus (HBV). It was prepared by two steps. First, 5'hydroxyl of L-FMAU was substituted by thioacetyl group using diisopropylazodicarboxylate(DIAD), Triphenyl phosphine(PPh3) and thioacetic acid in anhydrous THF. (omitted) -
We have developed the novel one-pot synthetic method for regioselective N-protected amines, carbamates as a protective group of amines, through the reaction of various ethers with chlorosulfonyl isocyanate (CSJ). This synthetic method provides a simple and convenient alternative for the formation of carbamates, such as -NHMoc, -NHPoc. -NHCbz, -NHPnz, -NHTroc and -NHAloc, by varying the alkyl moiety of ethers. (omitted)
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Extensive efforts in the search of therapeutically useful carbocyclic nucleosides have resulted in a wealth of their synthetic methodologies in racemic and optically active forms. The classical one-directional methods such as linear synthesis and convergent synthesis are the approaches most frequently seen in the literature for the preparation of carbocyclic nucleosides, and their advantages and limitations are well known. (omitted)
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The resistances to multiple antibiotics of strains of Gram-positive Staphylococci. methicillin-resistant Staphylo coccus aureus (MRSA), are now significant clinical problem. One of the major efforts of our laboratory has been the search and design and synthesis of novel lead compound for the purpose of obtaining highly potent anti-MRSA drug. Towards this end, we have recently reported the isolation of a potent anti-MRSA drug. (omitted)
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Lee, Bo-Young;Suh, Young-Ger;Lee, Yong-Sil;Min, Kyung-Hoon;Kim, Jin-Kwan;Seung, Ho-Sun;Park, Young-Ho 244.1
Advances in understanding of pain and analgesia have been made. Over the past few years, we have designed and synthesized a series of VR agonists, based on the structures of 12-HPETE and capsaicin. the natural VR agonist. But for the development of analgesic drugs, these synthetic VR agonists had problems like burning sensation. hypothermia. etc. So our recent studoes have focused on designs and syntheses of VR antagonists based on the structure of capsaicin(natural VR agonist), and capsazepine(synthetic VR antagonist). (omitted) -
For the development of new synthetic method for unnatural amino acid esters, alkyl
${\alpha}$ -anilinophenylacetates were synthesized through base-catalyzed hydrolysis of 1,5-diphenylhydantoins in methanol and O-alkylation of sodium${\alpha}$ -anilinophenylacetate with alkyl halides in DMF. Even though hydrolysis of hydantoin ring was undertaken under about 30-40$^{\circ}C$ in methanol, the hydantoic acid sodium salt was continuously converted to the sodium${\alpha}$ -anilinophenylacetate. (omitted) -
As part of our research to discover novel synthetic flavonoids which can be applied to chronic inflammation diseases, many structurally modified flavone analogs have been synthesized to obtain information concerning the relationships between structures and the anti-inflammatory activities. We previously reported that 7-methoxyflavone analogs generally exhibited strong inhibitory activities against cyclooxygenase-2 catalyzed prostaglandin production. (omitted)
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(+)-Brefeldin A (1) has been, since its isolation1 and structural elucidation2 many years ago, one of the most attractive targets for synthetic chemists due to its wide range of biological activities and well-functionalized macrolide structure. Its biological mode of action has been disclosed by a number of important discoveries. Especially the ability of brefeldin A to induce DNA fragmentation associated with apoptosis in cancer cells has stimulated a great deal of recent interest in its preclinical development as an anticancer agent. (omitted)
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Shin, Dae-Hong;Moon, Hyung-Ryong;Choi, Won-Jun;Lee, Kang-Man;Lee, Sang-Kook;Jeong, Lak-Shin 245.3
S-Adenosylhomocysteine hydrolase (SAH) catalyzes the hydrolysis of S-adenosylhomocysteine to adenosine and L-homocysteine and has been an attractive target for the development of broad spectrum antiviral agents. Based on the potent inhibitory activity of neplanocin A against SAH, we have reported the synthesis and novel mechanism of action of fluoro-neplanocin A. (omitted) -
Hetero chain compounds have high possibilities of being good medicinal candidate because of their well-known medicinal activity and relatively low subtitled carbon. By constructing the method of making this compound library, this research has the purpose to create a new medicinal candidate materials based on an easy medicinal search. The first step is to construct an Indole library in a compounding process with the design of a linker connecting a solid-state resin and a substrate. (omitted)
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Moon, Yoon-Soo;Basnet, Arjun;Zhao, Long-Xuan;Kim, Eun-Kyung;Lim, Hyun-Tae;Chae, Whi-Gun;Jeong, Tae-Cheon;Lee, Eung-Seok 246.2
It has been reported that 2-bromopropane might be a causative agent for reproductive toxicity and have immunotoxic effects. 1-Bromopropane known as an alternative to ozone depleting solvents, which has structural similarity to 2-bromopropane, has been reported to be neurotoxic to rats in long-term inhalation exposure. (omitted) -
PPAR-
$\gamma$ (Peroxisome Proliferator-Activated Receptor$\gamma$ ) 리간드들은 논문 조사를 통해 이루어졌다. PPAR-$\gamma$ 의 45개 알려진 화합물들을 찾았고, 12 생물활성 화합물을 선택했다. 리간드(rosiglitazone)과 단백질의 결합된 구조는 (1fm6)는 PDB로부터 획득했고, 단백질 coordinate를 가져와 PPAR의 활성 영역 잔기들은 확인했다. (2TYR, 1SER, 1HIS). CoMFA와 Flexi Dock을 통해 단백질과 리간드 사이의 상호작용과 결합에너지에 대한 상호 관계를 밝혔다. -
The three-dimensional quantitative structure-activity relationship (3D-QSAR) approach using comparative molecular field analysis (CoMFA) and comparative molecular similarity analysis (CoMSIA) was applied to 62 derivatives known as COX-2 selective inhibitors. Partial least square (PLS) analyses produced good predicted models with q2 value of 0.803 (s=0.285, F=215.401, r2=0.951) and 0.769 (s=0.192, F=245.364, r2=0.980) for CoMFA and CoMSIA, respectively. (omitted)
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Glucocorticoids are used most widely for the treatment of inflammatory bowel disease (IBD). For the efficient treatment and reduction of side effects, colon-specific delivery of a glucocorticoid is highly desirable. Previously, we synthesized prednisolone 21-sulfate sodium (PDS) as a colon-specific prod rug of prednisolone (PD) expecting that it might be stable and nonabsorbable in the upper intestine and hydrolyze in the colon to release PD. (omitted)
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The 18 ureidoceramide derivatives had been investigated for their cytotoxic activity against HT-29 colon cancer, Caki-2 renal cancer, A549 lung cancer, PC-3 prostate cancer, HL -60 leukemia cell using MTT assay. Cytotoxic activity was strongly influenced by the substituted alkyl chain length and the optimal alkyl chain length for cytotoxicity was C9-C12. (omitted)
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A series of tetrahydroaminoacridine and their analogues were synthesized. Tetrahydroaminoacridine(tacrine) is an anticholinesterase agent used in the treatment of Alzheimer's disease. Introduction of piperidine group at the para position enhanced anti-inflamatory activity for Alzheimer's disease. We investigated their ability to inhibit cyclooxygenase-1 and 2 isoforms. (omitted)
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Kim, Sun-Woo;Kim, Dong-Wook;Kim, Sun-Ho;Choi, Yeon-Joo;Kim, Joo-Young;Han, Mi-Jung;Kim, Oke-Kil;Kil, Kyong-Ok;Kim, Sung-Soo 249.1
The Korea Chemical Bank (KCB) has more than 80,000 compound collections. provided from many companies, academies and institutes. KCB has supported high-throughput screening (HTS) against 80 biological targets and identified a number of hits over 20 targets. These hits were first validated by confirming the purity and novelty of anticipated compound. We also determined their physiochemical properties. (omitted) -
3D-QSAR analyses by CoMFA and CoMSIA were conducted on a series of thiazole and triazole analogues with respect to their antifungal activities against Microsporum gypseum. A total of twenty analogues were used for the derivation of the 3D-QSAR models (training set). Thesuperposition of the compounds was performed by applying the FlexS with shape-based screening method. (omitted)
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In this work, we have conducted 3D-QSAR studies on a series of acanthonic acid derivatives that act as COX-2 inhibitors, using two different methods: comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA). CoMFA and CoMSIA analysis of twenty five pimarane analogues produced good models with high predictive abilities. (omitted)
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A series of rutaecarpine homologues were prepared from 2,3-polymethylene-4(3H-quinazolinones in 4 steps [i) PhCHO/Ac
$_2$ O, ⅱ) O,$_3$ ⅲ) PhNHNH$_2$ HCl, and ⅳ) PPA], in which dihedral angles of the two planar aromatic rings (indole and 4(3H)-quinazolinone) were controlled in a regular fashion. Their inhibitory activities on COX-1 and COX-2 were evaluated to show that the inhibitory activities were increased with the increase of the length of methylene unit while selectivities on COX-2 decreased leading a loss in trimethylene bridged system. -
A series of cinchona alkaloid-derived dimeric quaternary ammonium salts were prepared as chiral phase-transfer catalysts by the introduction of various functional groups on the phenyl ligand. Among them. the 2-F-substituted derivative 21 showed the highest enantioselectivity in the alkylation of the glycine anion equivalent 1 (97->99 % ee).
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(+)-Hernandulcin and (+)-4
${\beta}$ -HYdroxyhernandulcin was isolated as a sweet bisabolane sesquiterpene constituent of the Mexican plant Lippia dulcis Trev. (Verbenaceae) and has shown to be 1,000-1,500 times as sweet as sucrose. Natural (+)-hernandulcin was nontoxic when administered orally to mice and it did not induce bacterial mutation. (omitted) -
The 2,3-trimethylene-4(3H)-quinazolinone and 2,3-tetramethylene-4(3H)-quinazolinone are not the only alkaloids isolated from plants. but are the part of a family of intriguing alkaloids including the bronchodilator vasicinone, anti-endotoxic isaindigotone, cytotoxic luotonins, antibiotic tryptanthrin, and antiinflammatory rutacearpine as well as related alkaloids. (omitted)
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Jew, Sang-Sup;Lee, Jeong-Hee;Yoo, Mi-Sook;Lee, Yeon-Ju;Jeong, Byeong-Seon;Park, Boon-Saeng;Kim, Myoung-Goo;Park, Hyeung-Geun 252.1
Systematic investigations to develop an efficient enantioselective synthetic method for a-alkyl-alanine by the catalytic phase-transfer alkylation were performed. The alkylation of 2-naphthyl aldimine tert-butyl ester, 1 E with RbOH and O(9)-allyl-N-2'3'4'-trifluorobenzylhydrocinchonidinium bromide, 6, at \ulcorner5 \ulcorner\ulcorner showed the highest enantioselectivities, up to 96% ee. -
Hong, Chong-Hui;Kang, Chan-Soon;Choi, Bo-Kyung;Choi, Myoeng-Sin;Ko, Yong-Seok;Kim, Sang-Hyun;Jang, Seung-Jae;Lee, Kang-Chun 252.2
It was difficult that we analysed the polymeric drugs for the physico-chemical properties. Sodium hyaluronate is a linear polysaccharide composed of repeating disaccharides of sodium glucuronate and N-acetyl glucosamine found throughout the tissues of the body with high concentrations in the vitreous humor. synovial fluid and umbilical cord. It has a role in regulating the interaction between adjoining tissues. (omitted) -
Lee, Hong-Woo;Kim, Bok-Young;Ahn, Joong-Bok;Son, Hoe-Joo;Lee, Jae-Wook;Ahn, Soon-Kil;Hong, Chung-Il 252.3
An effective and convenient regioselective reduction of 5-benzylidene 2,4-thiazolidinedione derivatives to the corresponding 5-benzyl 2,4-thiazolidinedione derivatives has been accomplished using 3,5-dicarboethoxy-2,6-dimethyl-1,4-dihydropyridine (Hantzsch dihydropyridine ester: HEH) with silica gel as an acid catalyst in a good yield. -
Park, Hyeung-Geun;Park, Mi-Kyung;Choi, Ji-Yeon;Choi, Sea-Hoon;Lee, Ji-Hye;Suh, Young-Ger;Cho, Ha-Won;Oh, Uh-Taek;Lee, Jee-Woo 253.1
Twenty-seven N,N',N"-trisubstituted thiourea derivatives were prepared. Among them, 1- [3-(4'-hydroxy-3'-methoxy-phenyl)-propyl] -1,3-diphenethyl-thiourea (81, IC$\sub$ 50/= 0,32$\mu\textrm{m}$ ), showed 2-fold higher antagonistic activity than that of capsazepine (3, IC$\sub$ 50/= 0,65$\mu\textrm{m}$ ) against the vanilloid receptor in a Ca$\^$ 2+/ -influx assay. -
Jin, Jae-Ho;Kim, Gi-Hyun;Shin, Won;Shin, Ji-Soon;Choi, Jong-Yoon;Yoon, Sei-Ung;Kim, Min-Sung;Kim, Yang-Woo;Lee, Seung-Woo 253.2
National regulatory authority have the duty to ensure that available pharmaceutical products are of the required quality. This is particularly difficult for biotechnological products, the quality of which cannot be established entirely by test on the material in the final container. In general biotechnological products are distinguished from other drugs by being derived from genetically modified microorganism to humans, and frequently have a complex molecular structure. (omitted) -
Uhm, Young-Ho;Kim, Young-Doo;Seo, Eun-Seok;Kang, Tae-Hyuk;Kang, Dong-Hoon;Soh, Yun-Jo;Kang, Chul-Hun 254.1
CCl4 has been known as typical chemical which induce acute hepatitis accompanying increase in the levels of acute phase proteins in serum. In this study, after acute liver damage was induced by CCl4 in Sprague-Dawley rats, the levels of serum acute phase proteins were examined using 2-dimensional electrophoresis and lactic dehydrogenase (LDH), alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels in blood were also examined at 1, 2, 3 days after the induction to confirm acute hepatitis. (omitted) -
For many viruses, -1 ribosomal frameshifting regulate protein synthesis using an RNA pseudoknot. The integrity of pseudoknot stability and structure is the important feature for efficient frameshifting. Thus, small molecules interacting with viral RNA pseudoknots would be potential antiviral agents targeting\ulcorner frameshifting system in viruses. X-ray structure of RNA pseudoknot complexed with biotin has been reported, in which biotin is bound at the interface between the pseudoknot's stacked helices. (omitted)
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During our research program to find DNA strand-scission agents from higher plants, the MeOH extracts of the wood bark of Mucunar birdwoodiana Tutcher. (Leguminosae) exhibited the most potent activity with an IC
$\^$ 50/ value of 4.9$\mu\textrm{g}$ /$m\ell$ . Thus, detailed laboratory investigation was performed, and led to the isolation of the known compounds, catechin(1) and epicatechin(2) as the active principles. (omitted) -
Hong, Seong-Su;Han, Xiang-Hua;Jeong, Seon-Hwa;Park, Byung-Min;Lee, Seon-A;Lee, Kyong-Soon;Lee, Myung-Koo;Hwang, Bang-Yeon;Ro, Jai-Seup 255.2
Monoamine oxidase (MAO) is flavin-containing enzyme that catalyzes the oxidation of variety of amine-containing neurotransmitters such as catecholamines and serotonin to yield the corresponding aldehyde. Thus, MAO activity might play important roles in some pathological states of central nervous system diseases such as depression, alcoholism, and schizophrenia. (omitted) -
Marine Algae of order Chordariales are rich resources of bioactive metabolites. Methanolic extracts of the brown alga /shige Okamurae exhibited potent antioxidative and butyrylcholinesterase(BChE) inhibitory effects. Bio-guided purification [solvent partition, ODS flash, silica flash, gel-filtration on Sephadex LH 20, ODS HPLC] of them gave a compound 1. Its structure was elucidated by detailed analysis of spectroscopic data of 1 and comparison of literature data. A variety of bioassay for 1 is in progress.
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Han, Xiang-Hua;Hong, Seong-Su;Park, Seon-Soon;Huh, Jae-Doo;Lee, Kyong-Soon;Lee, Myung-Koo;Hwang, Bang-Yeon;Ro, Jai-Seup 256.1
As a part of our ongoing research to discover novel monamine oxidase (MAO) inhibitors of plant origin, we found that a MeOH extract from the whole plant of Cayratia japonica (Vitaceae) strongly inhibited the MAO activity in mouse brain. The EtOAc-soluble fraction was. therefore, subjected to the bioactivity-guided fractionations to isolate the active compounds. (omitted) -
Six known phenolic glycosides. hyperin(2), androsin(3), homoarbutin(4), isohomoarbutin(4a), pirolatin(7) and monotropein(6), together with two new compounds, (1)[mp. 215 - 217
$^{\circ}C$ , C$\sub$ 23/H$\sub$ 32/O$\sub$ 11/] and (5)[mp. 121 -123$^{\circ}C$ , C$\sub$ 18/H$\sub$ 26/O$\sub$ 8/] were isolated from the BuOH fraction of Pyrola japonica(Pyrolaceae). The structures of the known compounds were determined by chemical and spectroscopic methods. (omitted) -
Li, Gao;Xu, Ming-Lu;Seo, Chang-Seob;Kim, Hyo-Jin;Lee, You-Jeong;Lee, Yeun-Koung;Lee, Chong-Soon;Woo, Mi-Hee;Son, Jong-Keun 256.3
The bioactivity-guided fractionation of an active methylene chloride extract of the sclerotium of Poria cocos led to the isolation of compounds 1-5. These compounds were tested in the human colon carcinoma and human breast carcinoma cell lines, compounds 3, 4, and 5 exhibited IC50 values of 10.8, 15.4, and 5.1$\mu\textrm{g}$ /$m\ell$ against human colon carcinoma cell line. In addition, compounds 3, 4 and 5 showed moderate activities as inhibitors of Topoisomerase I and all compounds were inactive in the Topoisomerase II inhibition. -
Lee, Sung-Won;Li, Gao;Lee, Kyong-Sun;Jung, Jun-Sub;Xu, Ming-Lu;Seo, Chang-Seob;Song, Dong-Keun;Son, Jong-Keun 257.1
The bioassay-guided fractionation of preventive agents against lethality due to septic shock from the fruits of Illicium verum lead to the isolation of two known racemic mixtures of phenylpropanoids (1 and 2), along with two known phenylpropanoid glucosides (3 and 5) and two new phenylpropanoid glucosides (4 and 6). Their chemical structures were elucidated on the basis of spectroscopic studies. (omitted) -
Schizandra chinensis known as OMIJA belongs to Schizandraceae family, and is being used in the formulation of traditional medicine. Various column chromatographies with various solvent systems were used to isolate its compounds. To identify compounds isolated, instrumental analysis methods such as NMR and MS were employed. (omitted)
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The Dystaenia takeshimana (Nak.) Kitagawa is distributed in Ulreung island and it is an endemic species in korea. The MeOH extract from the root of D. takeshimana (Nak.) Kitagawa shows a good activity in anti-inflammatory assay (sPLA2IIA inhibition assay, COX-2 inhibition assay, 5-LO inhibition assay). (omitted)
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Rhus verniciflua STOKES (RVS) belongs to Anacardiaceae and grows Korea, China and Japan. distributed in the northeastern Asia. Rhus verniciflua STOKES has been used for anthelmintic medicine, stomachache, emmenagogue and constipation in oriental medicine. From the EtOAc fraction of 70% MeOH extracts, flavonoids were isolated by column chromatography using ODS, Sephadex LH-20 and silica gel. The structure of these compounds were identified on the
$^1$ H-NMR,$\^$ 13/C-NMR and FAB/MS spectroscopic methods. -
The Seeds of Astragalus sinicus(Leguminosae) is used for the treatment of excretion of urine, circulation of blood and the throat inflammation in Korean traditional medicine. Eight flavonoids were isolated from 80% Acetone extracts. The structure were elucidated as Quercetin 3-O-
${\beta}$ -D-Xylopyranosyl-(1\longrightarrow2)-${\beta}$ -D-galactopyranoside, ampelopsin and myricetin by phytochemical and spectral evidences. The other compounds are understudied by 2D-NMR. -
Kim, In-Kyum;Chin, Young-Won;Song, Won-Lim;Yang, Hye-Kyung;Kim, Young-Choong;Kim, Jin-Woong 259.1
In the course of hepatoprotective screening for domestic plants. the aerial parts of B. vulgaris var. cycla exhibited hepatoprotective activity which was determined by using the primary cultures of rat hepatocytes injured by H2O2. Bioactivity-guided separation for this plant gave a new flavonoid (1) and the known compounds (2-4), which structures were elucidated by 1H-NMR, HMQC, 1H-1H COSY and HMBC as compound 1, apigenin 8-C-, 7-O-di-$\beta$ -D-glucopyranoside, compound 2, vitexin 2"-O-$\beta$ -D-glucopyranoside, compound 3, (+)-dehydrovomifoliol, and compound 4, 3-hydroxy-5$\alpha$ , 6$\alpha$ -epoxy-$\beta$ -ionone. -
This study was carried out to isolate and to identify the compounds and to find out antioxidants from the leaf of Distylium racemosum which belongs to Hamamelidaceae family. To isolate compounds, leaf of this plant were extracted with 50% Acetone and then crude extracts was partitioned with hexane. ether and ethyl acetate (EtOAc) successively. After partitioned, EtOAc fraction was subjected to column chromatography with various solvent systems in silica gel and/or Sephadex LH-20. (omitted)
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Kim, Young-Sup;Park, Eun-Kyung;Heor, Jung-Hee;Kim, Seong-Kie;Kim, Jung-Sook;Choi, Yeon-Hee;Seo, Jee-Hee;Lee, Bong-Ho;Choi, Byoung-Wook 259.3
Alzheimer's disease(AD) is the most common cause of senile dementia in elderly people and the causes of AD are currently not fully understood. However, AD is generally understood to be associated with reduced levels of acetylcholine in the brain as cholinergic neurons are lost and cholinergic neurotransmission declines. There are growing evidences that two types of cholinesterase(ChE), i.e., acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) both play important roles in the regulation of acetylcholine level in brain and thus may have a crucial role in the development and progression of AD. (omitted) -
Magnoliae Flos(‘shin-j’). the flower buds of Magnolia kobus, is acrid to taste with a ‘warm’ property. It is a ‘wind-cold’ discutient and nasal decongestant and is principally used in the treatment of nasal congestion with headache, sinusitis and allergic rhinitis. By screening inhibitory activities on the melanin polymer biosysthesis in B-16 mouse melanoma cell lines, methylene chloride extract of Magnoliae Flos was found to have inhibitory effect on melanin polymer biosynthesis. (omitted)
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Min, Byung-Sun;Kim, Jung-Hee;An, Ren-Bo;Lee, Joong-Ku;Kim, Tae-Jin;Kim, Young-Ho;Joung, Hyouk;Lee, Hyeong-Kyu 260.2
Four known flavonoids and two galloyl glucoses isolated from the stem-bark of Juglans mandshurica (Juglandaceae), namely taxifolin (1), afzelin (2), quercitrin (3), myricitrin (4), 1,2,6-trigalloylglucose (5), and 1,2,3,6-tetragalloylglucose (6), were evaluated for their anti-complement activity against complement system. (omitted) -
Shim, Sang-Hee;Ryu, Ji-Young;Kim, Ju-Sun;Kang, Sam-Sik;Chung, Sang-Hun;Lee, Yeon-Sil;Lee, Sang-Hyun;Shin, Kuk-Hyun 261.1
The EtOAc and CH$_2$ Cl$_2$ soluble fractions from the fruit body of Ganoderma applanatum showed strong aldose reductase inhibitory activity. Nine compounds were isolated from both fractions. They were identified by spectral data as D-mannitol (1), 2-methoxyfatty acid (2), cerebrosides [(2S,3R,4E,8E)-1-O-${\beta}$ -D-glucopyranosyl-3-hydroxy-2-[(R)-2'-hydroxypalmitoyl]amino-9-methyl-4,8-octadecadiene] (3), daucosterol (4), 2,5-dihydroxybenzoic acid (5), protocatechualdehyde (6), 5-dihydroergosterol (7), ergosterol peroxide (8), and cerevisterol (9). (omitted) -
In the course of our researches for biologically active compound from Korean algae, purification of the methanolic extracts of two brown algae (Sagassum Sagamianum and Ishige Okamurae) collected off Jeju Island afforded an antioxidant polyphenolic compound (1). The molecular formular of 1 was established as C
$\sub$ 24/H$\sub$ 16/ O$\sub$ 13/ on the basis of the FAB mass and$\^$ 13/C NMR spectrum. (omitted) -
Lee, Seung-Jung;Kwon, Oh-Seung;Park, Eun-A;Ko, Sung-Kwon;Kim, Ha-Won;You, Byeong-Jin;Lee, Jae-Hee;Lee, Min-Won 262.1
Anti-tumor, anti-viral and anti-leukemic activity of cordycepin are well known. Adenosine was reported to induce an apoptosis in human leukemia cells. CM has been widely used as traditional medicinal herbs in China. Previously, we reported the results relating the isolation and characterization of cordycepin and adenosine from the cultured fruiting bodies of CM. We further studied the manufacturing process of CCCA for the prupose of developing anti-leukemic agents. (omitted) -
Han, Ah-Reum;Lee, Eun-Jin;Park, Go-Wooni;Windono, Tri;Jeohn, Gwang-Ho;Lee, Sang-Kook;Seo, Eun-Kyoung 262.2
Two phenylbutenoids, 4-(3',4'-dimethoxyphenyl)buta-1,3-diene (1) and 4-(2',4',5'-trimethoxyphenyl)buta-1,3-diene (2), were isolated from the roots of Zingiber cassumunar Roxb. (Zingiberaceae), as active constituents by bioassay-guided fractionation using a cytotoxicity assay against the HT1080 (human fibrosarcoma) cells. The isolates 1 and 2 exhibited a significant cytotoxicity with IC$\sub$ 50/ values of 0.71 and 0.74$\mu\textrm{g}$ /$m\ell$ , respectively, which are comparative to the positive control ellipticine (IC$\sub$ 50/=1.1$\mu\textrm{g}$ /ml). (omitted) -
Kim, Mi-Hee;Park, Eun-Jeon;Jun, Jung-Yang;Ko, Eun-Kyung;Park, Sung-Eun;Park, Sung-Uk;Sohn, Dong-Hwan;Kim, Youn-Chul 263.1
In order to find the new hepatoprotective agents from natural products, the isolation and identification of biological active components of the roots of Saururus chinensis has been carried out. A MeOH extract of this plant showed the significant hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells. Five lignans including sauchinone, manassantin A, manassantin B, saucerneol B, and di-O-methyltetrahydrofuriguaiacin B were isolated and identified by spectroscopic evaluation. (omitted) -
There is now increasing evidence that free radicals and active oxygen species are involved in a variety of pathological events. Free radical-mediated cell damage and free radical attack on polyunsaturated fatty acids result in the formation of lipid radicals. These lipid radicals react readily with molecular oxygen to produce peroxy radicals responsible for initiating lipid peroxidation. The peroxidation of cellular membrane lipid can lead to cell necrosis and considered to ve implicated in a number of pathophysiological conditions including liver disease. (omitted)
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In order to search for antioxidants from the plants, eighty-two kinds of herbal medicines were investigated. The MeOH extracts of Euryales Semen, Alpiniae Officinari Rhizoma. Drynariae Rhizoma, Sophorae Flos, Trachelospermi Caulis, Crassirhizomae Rhizoma, Euphorbiae lathyridis Semen, Lini Semen, Myristicae Semen, Epimedii Herba, Santali Lignum rubrum, Perillae Herba, Amomi Tsao-Ko Fructus and Garanii Herba showed potent antioxidative activities using the 1,1-diphenyl-2-picrylhydrazyl free radical generating system. (omitted)
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In order to search for the anti-HIV agents from natural products, Eighty MeOH extracts of medicinal plants were applied to a syncytia formation inhibition assay which is based on the interaction between the HIV-1 envelope glycoprotein gp120/gp41 and the cellular membrane protein CD4 of T lymphocytes. Among them, Ailanthus altissima showed a potent virus-cell fusion inhibitory activity. (omitted)
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The bark of Alnus japonica has been used of fever, hemorrhage and diarrehea in oriental traditional medicine. This research was focused on the anti-inflammatory activities of diarylheptanoid from the bark of A. japonica on RAW 264.7 cell line. Phytochemical examination of the bark of Alnus japonica Steudel had led to the isolation of ten diarylheptanoids. To investigate the anti-inflammatory activities of these compounds, nitric oxide and PGE2 production inhibitory in IFN-
${\gamma}$ , LPS stimulated RAW 264.7 cell were examined. (omitted) -
Low density lipoprotein (LOL) is the major cholesterol carrier in the blood stream. Also, LDL oxidation has been proposed as an important step in the formation of atherosclerotic lesion. Thus, protection of LDL from oxidation is needed to prevent or to retard the progression of atherosclerosis. In this study, 6-hydroxyeugenol was isolated from the methanolic extract of the Spiraea blumei and the sructure was elucidated by spectroscopic data analysis. (omitted)
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Diarylheptanoids [curcumin (1), demethoxycurcumin (2), bisdemethoxycurcumin (3), bisdimethoxymethylcurcumin (4), and 1,2-dihydrobis(de-O-methyl)curcumin (5)] were isolated from the methanolic extract of Curcuma longa L. and A new cyclic diarylheptanoiid (6) and a known compound 7 were isolated from fruits of Alnus japonica S. Diarylheptanoids (1-3) inhibited farnesyl protein transferase (FTPase) with an IC50 of 29-50
$\mu\textrm{m}$ . (omitted) -
Ecklonia stolonifera Okamura is a member of the family Laminariaceae, belonging to the order Laminariales. Previously we reported that the methanolic extract of the brown alga E stolonifera exerts antioxidative activity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical. In the course of a continuous study on the active principles of this alga, a new phlorotannin, named eckstolonol (2), was isolated along with the four known phlorotannins i.e. (omitted)
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Fruits of Hovenia dulcis T. (Rhamnaceae) was called ‘jiguja’ in oriental medicine which has been used for diuresis, remove of hangover and leaves has been used for detoxified the alcohol. In order to investigate the efficacy of antioxidative activity from leaves of Hovenia dulcis, the activity guided fraction and isolation of physiologically active substance were performed. Its 20%, 40%, 60%, 80%, 100% MeOH, H2O, Acetone fractions were examined antioxidative activity by DPPH method and TBARS assay. (omitted)
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The seeds of Astragalus sinicus grows in Korea have been used for oriental traditional medicine as the remedies for inflammation. Eight flavonoids were isolated from the Seeds of Astragalus sinicus and studied its anti-inflammatory activity. Some flavonoid compounds showed significant nitrogen monoxide(NO) production inhibitory activity in IFN-
${\gamma}$ , LPS stimulated RAW 264.7 cell. There compounds also showed significant antioxidative in DPPH assay. (omitted) -
In order to induce production of methylnissolin, sterol biosyntheis inhibitor, in the adventitious root of Astragalus membranaceus the effect of methyl jasmonate(MeJ), a growth regulator of plant, was investigated. After treatment of MeJ (0
$\mu\textrm{m}$ , 10$\mu\textrm{m}$ , 100$\mu\textrm{m}$ ) to the adventitious root which was harvested in the time interval of 0, 7, 14, 21, 28days and the fresh weight, dry weight and the contents methylnissolin was determined. (omitted) -
Chung, Mi-Yeon;Ko, Jeong-Suk;Ryu, Shi-Young;Jeune, Kyung-Hee;Kim, Koan-Hoi;Rho, Mun-Chual;Lee, Hyun-Sun;Kim, Young-Kook 267.1
Diacylglycerol acyltransferase (DGAT) is a microsomal enzyme that plays a central role in the metabolism of cellular glycerolipid. Recently, the generation of DGA T-deficient mice has provided a better understanding of triglyceride synthesis and its relationship to obesity. Therefore DGAT is an attractive target for treatments of triglyceride metabolism disorders, such as obesity or hypertriglyceridemia. (omitted) -
Melanin biosynthesis inhibitors are useful not only for the materials used in cosmetics as skin-whitening agents but also for the remedy of hyperpigmentation. In order to find the new skin-whitening compounds from the natural products. screening of tyrosinase inhibitory activity in vitro has been carried out. The EtOH extracts of two hundred crude drugs were performed at the concentration of 500
$\mu\textrm{g}$ /$m\ell$ . (omitted) -
Brazilin is the phenolic compound isolated from the Caesalpinia sappan. This compound has shown a wide range of physiological properties, such as hypoglycemic, anticonvulsant, vasorelaxing, and immunomodulating effects. In this study, we have found that brazilin induced DNA strand scissions in the presence of Cu(II) and this DNA cleavages were mediated by reactive oxygen species. (omitted)
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Prostaglandins (PGs) and NO (nitric oxide) are important elements to keep homeostasis and host defense system in human beings. When PGs and NO are overproduced by cyclooxygenase-2(COX-2) and inducible nitric oxide synthase (iNOS), respectively, they can cause chronic inflammation, tissue damage, and carcinogenesis. On this line, we are interested in finding agents that can inhibit the production of PGs and NO from natural products for devloping anti-inflammatory and cancer chemopreventive agents. (omitted)
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Polygonum cuspidatum has been used as treatments of dermatitis, inflammation, hyperlipidemia and diuretics in folk remedies. In order to evaluate the urinary effect of Polygoni cuspidati Radix, its MeOH extract was administerd in rats. We determined the total urin volume, chemical parameters(urea nitrogen, creatinine, uric acid), electrolytes(natrium, potassium, chloride) ) in serum and urin. Polygoni cuspidati Radix showed increase in urin volume and electrolytes.
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An extract of Alnus japonica (Betulaceae) cortex has been traditionally used for purifying blood, and curing feces containing blood, enteritis, diarrhea, alcoholism and cut wounds. In the preliminary test was carried out for determining whether it has the novel pharmacological activity, the butanol fraction showed significant inhibitory effect on carrageenan-induced paw edema as an acute inflammation, HCI.ethanol-induced gastric lesion and aspirin-ligation gastric ulcer. (omitted)
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CBNU-1 has been used as a folk medicine in India for general physical strengthening, anti-aging, blood sugar stabilization, urinary tract rejuvenation, enhanced brain functioning potency, kidney rejuvenation, immune system strengthening, arthritis, hypertension and many other application for numerous conditions. The present study was conducted to evaluate the possibility of CBNU-1 as fertility agent. (omitted)
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Enzyme-linked immunoassay system using monoclonal antibody (MAb) has become an important methodology for the quantitative and qualitative analysis of drugs and phytochemical compounds having small molecular weight. In this study, monoclonal antibodies against berberine, one of main constituent of Phellodendron amurense, Coptis japonica and Corydalis turtschaninovii, were produced. (omitted)
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Korean folk medicine ‘Bong Seon Wha Dai’ has been used to cure constipation and acute gastritis by meat. The botanical origin of the crude drug has never been studied pharmacogostically. To clarify the botanical origin of Bong Seon Wha Dai. the morphological and anatomical characteristics of Impatiens species growing in Korea, i.e. I. balsamina L., I. noli-tangere L.. I. textori Miq., I. textori Miq. forma. pallenscens Hara were studied. (omitted)
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In order to find the new hepatoprotective agents the preliminary screening of 12 prescriptions which have been used for the treatment of hepatic disease in Oriental traditional medicine has been carried out. Both DPPH free radical scavenging and hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells are performed. (omitted)
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The
${\gamma}$ - and${\beta}$ -secretase are one of the most important proteases, which cleave amyloid precursor protein (APP) into neurotoxic A${\beta}$ peptide in Azheimer's type dementia. In the course of screening for anti-dementia agents from natural products, the mycelial culture of mushroom Phellinus linteus showed potent inhibition againt${\beta}$ -secretase (BACE1). (omitted) -
Rhus verniciflua Stokes (RVS) is a widely used herbal plant with various biological properties. Our previous study using in vitro platelet aggregation in whole blood showed that the fractions of RVS had strong anti-aggregatory activity. In this study, using in vitro platelet aggregation in PRP and coagulation parameters, to investigate the anti-platelet activity and anticagulant effects of RVS ethyl acetate layer, the layer was subsequently fractionated by ODS columm chromatograph (50% MeOH). (omitted)
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Cornis fructus were extracted by successive extraction and then fractionated with hexane extract to get active fractions. This study was performed to determine the cytotoxic effect of hexane extract from Cornis fructus on NIH 3T3 fibroblasts and cancer cell lines using MTT assay. Hexane extract showed cytotoxic effect against A549, B16 melanoma and MDA-MB-231. Further fractionation with hexane extract were performed to obtain effective fraction, fraction 3 showed the cytotoxic effect against A549 and MDA-MB-231 cell line.
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Dopamine
${\beta}$ -hydroxylase (DBH) synthesizes norepinephrine from dopamine under the presence of ascorbate as a coenzyme. Dopamine is transported into the vesicles of the varicosity, where the synthesis and the storage of norepinephrine take place. Some drugs such as DBH inhibitors, dopaminergic agonists,etc. are known to assist in treating Parkinson's disease. (omitted) -
Dalwoneum is the one of Chinese traditional prescription used for the treatment of liver disease. This prescription consists of Arecae Semen (12 g), Magnoliae Cortex (9 g), Amomi tsao-ko Fructus (3 g), Anemarrhenae Rhizoma (12 g), Paeoniae Radix (9 g), Scutellariae Radix (12 g), and Glycyrrhizae Radix (3 g). Water extract of Dalwoneum showed the significant hepatoprotective effect on tacrine-induced cytotoxicity in Hep G2 cells. (omitted)
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Kim, S.H.;Eum, H.Y.;Lee, W.Y.;Park, S.W;.Lee, J.S.;Choi, S.M.;Kim, J.Y.;Jeong, W.Y.;Sim, S.H. 273.1
The CML -Ex is a traditional oriental medicine. The main constituents of CML-Ex are Rehmanniae Radix, Achyranthis Radix and Eucommiae Cortex. The objective of this study was to investigate the anti-inflammatory and analgesic activities of CML -Ex under various acute and chronic inflammatory and analgesic models. The drug was orally administered at 30, 100, 300 and 600 mg/kg body weight. (omitted) -
The present study was designed to evaluate central inhibitory effects of an essential oil from Acori graminei Rhizoma (AGR), the dry rhizomes of Acorus gramineus Solander (Araceae) upon fragrance inhalation (aroma therapy). Preinhalation of an essential oil of AGR markedly delayed the appearance of pentylenetetrazole-induced convulsion. Furthermore, the inhalation of an essential oil of AGR impressively inhibited the activity of
${\gamma}$ -aminobutyric acid (GABA) transaminase, a degradating enzyme for GABA as inhalation period is lengthened. (omitted) -
To elucidate the effect of bioconversioned ginseng(Sun ginseng) and its butanol fraction on adenine-induced renal failure. rats were fed ad libitum on diet containing 0.75% adenine for 20 days to induce renal failure, and bioconversioned ginseng was orally administrated during the feeding period. On days 10 and 20, BUN, Creatinine, Ca and P contents were analyzed in serum and urine, and on days 20, BUN, Creatining, Ca and P contents were analyzed in serum and urine, and on days 20, blood pressure, hear pulse and relative kidney weight were measured. (omitted)
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Jung, Dae-Young;Lee, Ho-Young;Ha, Hye-Kyung;Jung, Da-Young;Yang, Ha-Ru;Lee, Je-Hyun;Kang, Sam-Sik;Kim, Chung-Sook 274.2
The aim of this study was designed to determine the induction of rat growth hormone(rGH) by extracts of a popular herb, Glycyrrhizae radix(GR), roots of Glycyrrhiza glabra$\sub$ Linne/, and Glycyrrhiza uralensis$\sub$ Fischer/. In vitro study was carried out using primary rat pituitary cell culture for 3 days and then was treated with methanol extract corresponding to 1 mg of dried weight of herb per 1$m\ell$ of culture solution. (omitted) -
Because people who take more than two drugs have increases, a simple and sensitive method for the simultaneous analysis of amphetamine, methamphetamine and nalbuphine in urine was developed. After alkalinization of the urine samples with 6 N-NaOH, the analytes were extracted using ethyl acetate, derivatized with MSTFA : TSIM : TMCS (= 100 : 2 : 5) prior to gas chromatography-mass spectrometry(GC-MS) analysis with selected ion monitoring. (omitted)
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Several
${\beta}$ -agonists were investigated for the possible separation of the enantiomers by reversed-phase high-performance liquid chromatography after derivatization with a new chiral derivatization agent, GATC. The derivatization proceeded quantitatively within 1 h at room temperature. The corresponding diastereomers were well resolved an ODS column with acetonitrile-acetate buffers a mobile phase and monitored at UV 254nm. (omitted) -
This study describes a simple and sensitive semi-micro HPLC method with UV detection and direct deproteinization. The plasma protein was precipitated using perchloric acid (60%) and the supernatant was directly injected onto the semi-micro HPLC system. The separation was achieved on a C18 (25 mm
${\times}$ 2.0 mm I.D) analytical column with a mobile phase of sodium acetate buffer (pH 3.5, 50 mmol) - acetonitrile (60:40, V/V). (omitted) -
Simultaneous enantioseparation of nine racemic non-steroidal antiinflammatory drugs (NSAIDs) for their accurate chiral discrimination was achieved by cyclodextrin (CO) modified capillary electrophoresis in the normal polarity (NP) mode and in the reversed polarity (RP) mode. The NP mode employed neutral tri-O-methyl-
${\beta}$ -cyclodextrin (TM${\beta}$ CD) as a selector dissolved in MES buffer (PH 6.0). (omitted) -
Chang, Soo-Hyun;Jang, Seung-Jae;Choi, Don-Woong;Kim, Mi-Jeong;Kim, Hee-Sung;Jung, Ki-Sook;Chang, Seung-Yeup 276.3
A simple, accurate GC analytical technique for the determination of phthalates. commonly used as plasticizers during the manufacturing process of PVC bags, in blood component preparations was developed and validated. The blood component preparations were extracted with n-hexane. The n-hexane layer was evaporated to dryness and the residue was dissolved in 1$m\ell$ of n-hexane and analyzed by GC and GC/MS. (omitted) -
A high-performance liquid chromatographic method using the liquid extraction procedure was developed for the determination of L -FMAUS. a new L -FMAU derivative, in rat plasma and urine using 3-aminophenyl sulfone as an internal standard. A 100-
${\mu}\ell$ aliquot of distilled water containing the L -cysteine (100 mg/$m\ell$ ) was added to a 100-${\mu}\ell$ aliquot of biological sample. L-Cysteine was employed to protect binding between 5'-thiol of l and protein in the biological sample. (omitted) -
A liquid chromatography-tandem mass spectrometric (LC/MS/MS) method for the determination of tiropramide in human plasma was developed. Tiropramide and internal standard, cisapride were extracted from human plasma with MTBE at basic pH. A reverse-phase LC separation was performed on Luna C8 column with the mixture of acetonitrile-ammonium formate (10 mM, pH 4.5) (5:5, v/v) as mobile phase. (omitted)
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Recently, particular attention has been paid to the chiral separation of amino acid enantiomers because of their different biological activities. Hence, the high optical purity of aromatic amino acids is critical because of their important functions in the central nervous system. For the accurate chiral discrimination. we attempted to exploit the crosschecking each enantiomeric migraion orders of aromatic amino acids measured using (+)-18C6H4TA and (-)-18C6H4TA as the chiral selectors under pH 2.0, tris/citric acid buffer.
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A column-switching semi-micro HPLC method with fluorescence detection was developed for the direct analysis of rebamipide in human plasma. Plasma was filtered through a 0.45
$\mu\textrm{m}$ membrane filter and 5${\mu}\ell$ of the filtrate was directly injected onto the pre-column. After elution of the plasma proteins to waste, the retained rebamipide and internal standard(ofloxacin) were transferred to a C18 semi-microcolumn (5$\mu\textrm{m}$ , 150${\times}$ 2.0mm) where they were separated using acetonitrile-1.4% acetic acid (40:60, v/v) as mobile phase. (omitted) -
A chiral stationary phase (CSP) prepared by bonding (18-crown-6)-2,3,11,12-tetracarboxylic acid (18-C-6-TA) to aminopropyl silica gel by HPLC was used in resolving several racemic drugs containing primary amino moiety. Most compounds used in this study were resolved on the CSP using 80% methanol in water (V/V) containing 10mM sulfuric acid as a mobile phase. These results on the CSP were compared to those on the similar CSP derived from 18-C-6-TA of the same chiral selector by different connecting method.
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Kim, Do-Hyung;Lim, Hun-Rang;Woo, Young-Ah;Kim, Hyo-Jin;Kang, Shin-Jung;Choi, Hyun-Chul;Choi, Han-Gon 279.1
NIR reflectance spectroscopy, using a fiber-optic probe was used to determine rapidly and non-destructively the content of ambroxol in intact ambroxol 30 mg (nominal content 12.5% m/m ambroxol) tablets by collecting NIR spectra in range 1100 - 1750 nm and using PLSR calibration method. The tablets (10.3 - 15.9% m/m ambroxol, i.e., 82 - 127% of the nominal label content) were used 7 calibration set and 5 validation set. (omitted) -
A simple and accurate reverse-phase high performance liquid chromatography (HPLC) coupled with photodiode array was developed for the determination of dextromethorphan(DM) and its metabolite dextrorphan(DX) in human urine. Chromatographic separation was accomplished on a cyano analytical column at 220 nm using a mobile phase containing 25 mM triethylammonium phosphate buffer(PH 3.0) in a 0-70% ACN gradient and triazolam(TZ) was used as internal standard(I.S). (omitted)
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Ko, Yong-Seok;Jang, Seung-Jae;Kang, Chan-Soon;Choi, Bo-Kyung;Kim, Hye-Soo;Kim, Eun-Jung;Cho, Myoeng-Sin;Hong, Chong-Hui;Kim, Sang-Hyun 280.1
The high-performance liquid chromatography method was performed for test method development of related compounds in pharmaceuticals. Using reverse-phase column and gradient elution of 1 % acetonitrile-acetonitrile: H20:triethylamine (70:30:0.5), lansoprazole, 2-hydroxybenzimidazole, 2-mercaptobenzimidazole, lansoprazole sulfone, lansoprazole sulfide could be individually identified and quantitated. (omitted) -
The applicability of liquid chromatography-atmospheric-pressure chemical-ionization mass spectrometry (LC-APCI-MS) for the determination of 13C-urea in 13C-urea/PEG capsules has been studied. It is essential to assess the stability of a newly developed low-dose (38 mg) 13C-urea/PEG capsule. which will be used for 13C-urea breath test (13C-UBT) to detect Helicobacter pylori infection. (omitted)
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Kim, Young-Ok;Jang, Jung-Yun;Lee, Jeong-Pyo;Yang, Seong-Jun;Lee, Kyung-Shin;Yang, Won-Jun;Kim, Chong-Kap;Choi, Sang-Sook 280.3
A high-performance liquid chromatographic method for the simultaneous quantitative analysis of DMDM hydantoin, sorbic acid, phenoxy ethanol in cosmetics was studied by using a X-terra C18 column and 0.75mM KH2PO4 in 0.85% sulfuric acid and methanol mixture(7:3) at 214nm. Calibration curves were found to be linear in the 20-100$\mu\textrm{g}$ /mL range (DMDM hydantoin), 50-250$\mu\textrm{g}$ /mL range (sorbic acid) and 10-50$\mu\textrm{g}$ /mL range (phenoxy ethanol). The result of recovery test were 96.6% - 104.2%. This HPLC method can be applied quality control of cosmetics. -
Purpose. The purpose of this study was to develop and validate sensitive and specific analytical method for determinination of simvastatin in human plasma by the column-switching high-performance liquid chromatography (HPLC) system with UV detection. Methods. Simvastatin and internal standard were extracted into diethyl ether from plasma. (omitted)
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Recently, ‘bokbanggamchopyeon’, chinese analgesic which is carried in korea by travelers becomes a problem when they pass customs because it contains opiate alkaloids morphine and codeine. At this time, opium is assigned as narcitics in korea according to the rule concerning narcotics control, and its major component morphine and codeine too. (omitted)
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This study established a sensitive novel Quantification method for detecting glimepiride in human plasma using LC-MS/MS for pharmacokinetic studies. The mobile phase used after degassing was composed of 10 mM ammonium acetate and acetonitrile (20:80, pH 3.0), with flow rate of 200uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)
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The carboxylated acidic non-steroidal antiinflammatory drugs (NSAIDs) constitute the principal class of agents for controlling the pain and inflammation of the rheumatic diseases. It is mostly administered as a racemic mixture like most other drugs with asymmetric carbon atoms. However enantiomers of many racemic drug substances have been shown to posses different pharmacological toxicological properties. (omitted)
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Lee, Dong-Mi;Won, Young-Jun;Yoon, Chang-Yong;Seo, Il-Won;Nam, Hye-Seon;Park, Dong-Hee;Lee, Hyang-Mi;Kim, Se-Sil;Jung, Eun-Mi 283.1
This study was designed to develop and validate an isocratic reversed phase high performance liquid chromatographic(HPLC) method for the quantitation of sobrerol in drug preparations, and obtain the data pool that can be used in the revision of pharmacopoeia. The separation of sobrerol and the other compounds (S-carboxymethylcysteine, acetaminophen, methyl paraben, propyl paraben, and sobrerol degradants) was achieved in a C18 column with an acetonitrile-methanol-water(24.5:10.5:65.0) mobile phase. (omitted) -
This study established a highly sensitive novel quantification method for detecting felodipine in human plasma using LC-MS/MS. The mobile phase used after degassing was composed of 1 mM ammonium acetate and acetonitrile (20:80, pH 6.0), with flow rate of 200 uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)
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Paik, Man-Jeong;La, Sook-Ie;Lee, Yoon-Suk;Kim, Ji-Yung;Choi, Young-Me;Kuon, Do-Won;Kim, Jung-Han;Kim, Kyoung-Rae 284.1
Modified nucleosides and polyamines excreted in urine are well-known as biochemical markers for cancer. The metabolomics on the urinary nucleosides and polyamines is thus gaining interest in the cancer study. In this study, the levels of nucleosides and polyamines in urine samples from cancer patients under acupuncture treatment were determined by high resolution capillary electrophoresis and gas chromatography, respectively. (omitted) -
Using a column-switching technique. highly sensitive and selective semi-micro high-performance liquid chromatographic (HPLC) method has been developed for the determination of baclofen in human plasma. Following precipitation of plasma sample containing baclofen with zinc sulfate-acetonitrile, samples were directly injected on to the system. (omitted)
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Talniflumate is a potent analgesic and anti-inflammatory drug widely prescribed in rheumatoid diseases. The purpose of this work was to develop and validate a specific and robust method for the simultaneous determination of talniflumate and its metabolite, niflumic acid, in human plasma. Indomethacin was used as an internal standard (IS). (omitted)
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ChiroSil RCA(+) and SCA(-) HPLC chiral stationary phases (CSPs) developed by covalently bonding (+)- and (-)-(18-crown-6)-2,3,11,12-tetracarboxylic acid (18-C-6-T A) to silica gel were employed for enantioresolution of racemic amino compounds, respectively. Also, these 18-C-6-TA covalently bonded CSPs were compared to a commercially available Crownpak CR CSP prepared by coating chiral crown ether as a chiral selector on ODS column. (omitted)
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Analysis of illicit methamphetamine samples seized in Korea is discussed. The samples are extracted with the small portion of ethyl acetate under neutral conditions and the extracts are analyzed by GC-MS. Several impuritiy peaks are found in each chromatrogram. Eight compunds (1,2-Dimethyl-3-phenylaziridine, amphetamine oxime, ephedrine, N-formylmethamphetamine, N-acetylmethamphetamine, acetylephedrine, 3,4-dimethyl-5-phenyl-2-oxazolidone, methamphetamine dimer) are identified impurities in illicit methamphetamine and the identity of the impurity is conformed synthesis. (omitted)
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Cho, Hee-Yeong;Yun, Cheol-Won;Kong, Jae-Yang;Kim, Kyoung-Soon;Park, You-Mie;Lee, Sang-Hyun;Kim, Bak-Kwang 286.1
Chrysin, a natural flavone compound contained in plants. has anti-inflammatory activity. Its anti-inflammatory effect has been previously explained in part by the suppression of promoter activities of inducible pro-inflammatory enzymes (cyclooxygenase-2 (COX-2) and inducible nitrogen synthase (iNOS)). Nitrate production triggered by the activation of lipopolysaccharides (LPS) was most highly suppressed by the treatment of chrysin, follwed by 5-hydroxy-7-methoxyflavone (Ch-2), 5,7-diacetylflavone (Ch-4) in cultured Raw 264.7 cells. (omitted) -
Ji, Hye-Young;Kim, Sook-Jin;Lee, Hong-Il;Lee, Seung-Seok;Lee, Dong-Ha;Lim, Hong;Lee, Hye-Suk 286.2
The purpose of this paper was to identify the metabolic pathway of a new neuroprotective agent, KR-31543 for ischemia-reperfusion damage in human liver microsomes and characterize cytochrome P450 (CYP) enzymes involved in the in vitro metabolism of KR-31543 generates two metabolites in human liver microsomes : M1, N-(4-chlorophenyl)-N-(2-methyl-2H-tetrazol-5-ylmethyl)amine and M2, hydroxy-KR-31543. (omitted) -
F
$_2$ -isoprostanes are derived in vivo principally from the formation of positional peroxyl radicals of arachidonic acid, endocyclization to prostaglandin G$_2$ -like structures, and reduction to PGF$_2$ -like compounds. F$_2$ -isoprostanes have been proposed as biomarkers of lipid peroxidation, oxidative stress status, and oxidation of low density lipoprotein (LDL) in atherogenesis. Especially, elevated 8-iso-PGF$\sub$ 2a/ is known as a useful clinical biomarker of oxidative stress in-end stage renal disease (ESRD) patients receiving hemodialysis (HD). (omitted) -
Jung, Soon-Ja;Jung, Ji-Hyun;Cao, Li-Hua;Shin, Young-Hee;Son, Jong-Keun;Lee, Chong-Soon;Woo, Mi-Hee 287.2
Rubia akane (Rubiaceae) is a perennial vine plant and generally grows at the mountain, field and fence of Korea, Japan, China and Taiwan. This plant grows about two meters and has empty stem and red roots. The roots of this plant have been used as a Korean traditional medicine for the treatment of cough, the stone in the bladder and kidney, inflammation of the joints, uterine hemorrhage and uteritis. (omitted) -
Ze, Keum-Ryon;Park, Sang-Young;Cho, Chang-Hee;Sung, Rak-Sun;Lee, Jong-Pil;Park, Ju-Young;Cho, So-Yean;Jin, Zhexiong;Kim, Jun-Hyuk 288.1
The determination method of decursin and decursin angelate from Angelicae gigantis Radix, an important crude drug in oriental medicine, was developed and validated by a reverse-phase liquid chromatography. The decursin and decursin angelate, the structural isomer aspyranocoumarin each other, are the main organic constituents in Angelicae gigantis Radix. (omitted) -
Kim, Kyoung-Soon;Lee, Sang-Hyun;Lee, Yeon-Sil;Jung, Sang-Hoon;Park, You-Mie;Shin, Kuk-Hyun;Kim, Bak-Kwang 288.2
The anti-oxidant activities of the various fractions from the herbs of Artemisia apiacea were investigated. The n-hexane and n-butanol fractions were found to cause significant free radical scavenging effects on DPPH, their scavenging potencies as indicated in IC50 values, being 230.1 and 183.7 mg/$m\ell$ , respectively. (omitted) -
Sphingolipid species are important second messengers due to their role in the mitogenesis, differentiation and apoptosis. We developed a new column liquid chromatography-triple quadrupole tandem mass spectrometry (LC-MS/MS) in combination with multiple reaction monitoring (MRM) method for the rapid, simultaneous and quantitative determination of unambiguous detecting sphingolipids in cell culture of human cancer cells (HL-60). (omitted)
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EVALUATION OF NON-INVASIVE BLOOD GLUCOSE MEASUREMENT USING THREE TYPES OF NEAR INFRARED SPECTROMETERThree types of near infrared spectrometer, a photo diode array type, a dispersive type and a FT type, were evaluated and compared the systematic difference in blood glucose measurement. The fundamental study was performed by adding glucose to buffer solution and bovine blood as the preceding study of non-invasive blood glucose. Spectra were collected using a 1.0 mm optical pathlength quartz cell by transmittance method. (omitted)
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The aim of this work was to develop an reverse-phase method for the analysis lysozyme contents. This method was sensitive and reproducible. The experimental samples were 8 kinds of capsules and one tablet. collected in domestic area. The results were summarized as follows. (omitted)
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Oxidative DNA damage has been associated with many disease. Quantation of DNA adducts is considered to be a useful biomarker of oxidative DNA damage because its formation can also be induced by oxidative stress. Extensive efforts have been taken to identify the analytical methods for minimizing the artifactual formation of oxidative DNA damage. We have done direct analysis of DNA adducts using LC/ESI-MS without urine sample extraction. (omitted)
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Skin Moisture is an important factor in skin health. Measurement of moisture content can provide diagnostic information on the condition of skin. In this study, a photo diode array type near infrared spectroscopy was used to determine skin moisture. Diffuse reflectance spectra were collected and transformed to absorbance using 1-nm stepsize over the wavelength range of 1100 nm to 2200 nm. (omitted)
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Hong, Ji-Youn;Hong, Jee-Eun;Lee, Eun-Ah;Park, Song-Ja;Lho, Dong-Seok;Kim, Jong-Hyun;Choi, Myung-Ja 290.3
To increase detection sensitivity for multi-DDT residues (o,p-/p,p-DDT, o,p-/p,p-DDE, o,o-/o,p-DDD) analysis, a highly selective sample clean-up method was introduced prior to GC/MS analysis using immunoaffinity column. The immunoaffinity matrix was prepared by coupling IgG fraction of DDT antiserum to cyanogens bromide activated Sepharose 4B. Three DDT antisera (DDA-1, DDHP-2, DDCP-3) were test for affinity column ligand that obtained by imunizing respective DDT immunogen to rabbits, and IgG was purified using protein A affinity purification. (omitted) -
The purpose of this study is to provide KFDA's guidance for premarket notification submission and labeling for prescription use drugs of abuse in vitro diagnostic devices. To evaluate in vitro diagnostic devices the following performance characteristics should be described in detail within the submission: analytical sensitivity or minimum detection limit, cutoff concentration, specificity and cross reactivity, interference, precision, method comparison and stability. (omitted)
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The purpose of this study was to investigate the transport characteristics of passage cultured l1uman nasal epithelial cell monolayers grown on Transwell@ inserts using liquid-covered culture (LCC) method. The monolayer of passage 2 and 3 exhibited tight barrier (TEER>1,000 ohmxcm
$^2$ ) in 2-3 days after seeding. In the morphological studies by actin staining and SEM/TEM, the existence of tight junction was clearly observed. (omitted) -
Purpose. To develop a new heterodisperse 650mg acetaminophen HPMC matrix tablet with biphasic sustained release profiles. Methods. Hydroxypropylmethylcellulose(HPMC) matrix tablets were prepared by wet-granulating drug with other excipients, followed by direct compression of the dried granule mixtures into tablet using a rotary tablet machine. (omitted)
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In the gene therapy. viral gene delivery systems are limited in use because of several drawbacks like host immune reactions. Hence, non-viral gene delivery systems such as cationic polymers or synthetic gene carriers are being widely investigated to overcome the problems in the use of viral vectors. We synthesized a new conjugate of polyethyleniminet carrying galactose moieties as a targeting ligand for asialoglycoprotein (ASGP) receptors of hepatocytes. (omitted)
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Kim, Su-Youn;Lee, Yeon-Joo;Lee, Hyung-Won;Lee, Hyo-Jung;Lee, Seung-Yeon;Youe, Jee-Sun;Oh, Seaung-Youl 293.1
Electroosmotic flux during iontophoresis originates due to the net negative charge of the current passing channels (pores) in skin at physiological pH (pH 7.4). Thus, the channels are permselective to cations, and this causes the convective solvent flow from anode to cathodal direction. This solvent flow facilitates the flux of cations (from anode), inhibits that of anions (from cathode), and enables theenhanced transport of neutral, polar solutes. (omitted) -
Topical buccal therapy with steroid anti-inflammatory drugs is based on the concept that a high activity of steroids can be produced at the site of administration and, at the same time, the degree of systemic side effects can be minimized or avoided. In this study we developed a new formulation consisting of a mucoadhesive bead for buccal administration of glucocorticoids. (omitted)
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At pH 7.4 (physiological pH), skin is permselective to cations, due to the net negative charge of the current passing channels (pores) in skin. This causes the convective solvent flow (electroosmotic flow) from anode to cathodal direction. In this work, we have investigated several factors (pH. current density and ionic strength) that can affect the electroosmotic flow. (omitted)
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Gentisic acid, a skin-whitening agent, is known to possess tyrosinase inhibition activity. In order to develop an effective skin-whitening agent, hydroquinone derivatives in which the carboxylic acid moiety of gentisic acid was replaced with various functional groups, were selected and evaluated for their ability to inhibit tyrosinase activity as well as to inhibit melanin release. (omitted)
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A suitable model for the estimation of the drug release from nanoparticles has been varied and problematic, especially for the release from lipid nanoparticles containing water-insoluble drugs, due to the difficult particle collection from the release medium. Dialysis membrane has been widely used for the release test from colloidal carrier systems. The amount of drug from the carriers in normal dialysis diffusion technique was very low typically. (omitted)
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Lipid nanodispersion (LN) composed of biocompatible lipids and surfactants is an alternative parenteral drug delivery system especially for lipophilic drugs. It has been studied for versatile applications such as oral, parenteral, topical, ocular, vaccine, and peptide drug delivery. The purpose of this study was to produce a novel LN system for intravenous injection using the high pressure homogenization. (omitted)
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Kim, Hee-Kyu;Kim, Jong-Seok;Lee, Sang-Kil;Yang, Sung-Woon;Lee, Ji-Eun;Choi, Han-Gon;Yong, Chulsoon;Choi, Young-Wook 296.1
Purpose. External gel formulations of prostaglandin E1 ethyl ester (PGE1-EE), a prod rug of PGE1 as a therapeutic agent for erectile dysfunction, were tried and evaluated by in vitro skin penetration characteristics and in vivo pharmacodynamic effects in cat. Method. The in vitro skin penetration was performed with Franz diffusion cell and examined in aspects of alcohol/polyol ratios and various enhancers. (omitted) -
Carduus marianus extract (formally called silymarin) have been used mainly as a medicament for hepatobiliary diseases. The major component of silymarin is silybin, which constitutes between 50 and 70% of the drug and is the major active component. Many experiments show the efficacy of silybin parenterally administerated. But, its bioavalability is low after oral administration due to its low solubility in water. (omitted)
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Organic solvent-based enteric coating technology using hydroxypropyl methylcellulose phthalate (HPMCP) has been developed for many years due to low water solubility of HPMCP. In this work, aqueous HPMCP nanoparticles (HPMCP-NPs) were prepared by neutralization emulsification method using HPMCP powder and ammonium hydroxide (NH40H) in the absence of any organic solvent and emulsifier. (omitted)
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Park, Eun-Jeon;Nan, Ji-Xing;Zhao, Yu-Zhe;Lee, Sung-Hee;Kim, Young-Ho;Nam, Jeong-Bum;Lee, Jung-Joon;Sohn, Dong-Hwan 297.2
The roots and rhizome of Acanthopanax koreanum are used as folk medicine to ameliorate hepatitis in Korea. The ability of A. koreanum to protect mice from fulminant hepatitis induced in mice by D-galactosamine and lipopolysaccharide was evaluated. Preparations of A. koreanum used were an ethanol extract, and the ethanol-soluble and ethanol-insoluble components of the water extract. (omitted) -
Park, Eun-Jeon;Nan, Ji-Xing;Zhao, Yu-Zhe;Lee, Sung-Hee;Kim, Young-Ho;Nam, Jeong-Bum;Lee, Jung-Joon;Sohn, Dong-Hwan 298.1
The aim of this study was to investigate the protective effect of acanthoic acid on liver injury induced by either tertiary-butyl hydroperoxide (tBH) or carbon tetrachloride in vitro and in vivo. Acanthoic acid, (-)-pimara-9(11),15-diene-19-oic acid, is a diterpene isolated from the root bark of Acanthopanax koreanum. In in vitro study, the cellular leakage of lactate dehydrogenase (LDH) with 1.5 mM tBH for 1 j, were significantly inhibited by treatment with acanthoic acid(25 and 5mg/mL). (omitted) -
The insulinotropic hormone, glucagons-like peptide-1 (GLP-1), which has been proposed as a new potential therapeutics for type-II diabetes, but this is metabolized extremely rapidly by the ubiquitous enzyme, dipeptidyl peptidase IV (DPP IV), forming a metabolite, which acts as an antagonist at the GLP-1 receptor. (omitted)
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Multivesicular DepoFoam technology is best suited for the encapsulation and sustained release of water-soluble drugs. The purpose of the present study was to prepare multivesicular DepoFoam particles and investigated possibility of oral delivery of a peptide, human epidermal growth factor (rhEGF). The multivesicular DepoFoam particles containing rhEGF was prepared by a two step water-in-oil-in-water double emulsification process. (omitted)
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Various bupivacaine-Ioaded microspheres were prepared with poly (d,l-Iactide) (PLA) by solvent extraction method. The internal solution of polymer(PLA R104) and drug in glacial acetic acid was introduced into the external phase of polyvinylpyrrolidone (PVP K-30) in polyethyleneglycol (PEG), and emulsified to be an oil-in-oil (o/o) emulsion. The o/o emulsion was poured to the buffer solution. (omitted)
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Salmon calcitonin (sCT) is a therapeutic polypeptide hormone consisting of 32 amino acids (3432 Da). As with other bioactive peptide therapeutics, however, therapeutic use of sCT has been limited due to the problems of short circulating half-life and rapid proteolytic degradation. To get over this problem, the three positional isomers of mono-PEGylated sCT were prepared and among these, the best drug candiate for nasal application was chosen. (omitted)
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Unlike cationic liposome/DNA complexes, neutralliposomes containing plasmid DNA are stable in blood and does not selectively entrapped in the lung. The objective of this study was to construct neutral liposomes containing plasmid DNA with optimal encapsulation efficiency. Plasmid DNA (pGL2 clone 753,-6 kb) was encapsulated by the freeze/thawing method into liposomes composed of 1-palmitoyl-2-oleyl-sn-glycerol-3-phosphocholine(POPC), didodecyldimethylammonium bromide(DDAB), distaroylphosphatidyl-ethanolamine polyethylene glycol 2000(DSPE-PEG 2000) and DSPE-PEG 2000-maleimide. (omitted)
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Lee, Sung-Hee;Choi, Jeong-Yong;Park, Eun-Jeon;Zhao, Yu-Zhe;Park, Young-Nyun;Chae, Keon-Sang;Sohn, Dong-Hwan 300.3
The activation of the hepatic stellate cell (HSC) is a key step in liver fibrogenesis. Utilizing large scale sequencing of a 3' -directed cDNA library, we investigated expression profiles of quiescent and activated rat HSCs. During the activation process, O-acetyl disialoganglioside synthase (OAcGD3S) was identified as one of the significant upregulated factors. Upregulation of OAcGD3S in cultured HSCs was confirmed by both northern and western blot analyses. (omitted) -
Kim, Mi-Jeong;Chang, Sung-Jae;Choi, Don-Woong;Kim, Hee-Sung;Chang, Soo-Hyun;Jung, Ki-Sook;Kim, Ji-Ha;Choi, Jong-Won;Chang, Seung-Yeup 302.1
Accelerated stability testing was performed on the different 7 dosage forms in order to evaluate the influences of the existence of other vitamins, minerals, excipients on the chemical stability of vitamin A in complicated vitamin drug products. The stability results suggested that increasing of storage time and temperature has resulted in increasing the rate of vitamin A decomposition and the shelf lives(t$\sub$ 90/) under the test decreased as the storage temperature increased. (omitted) -
For polymeric material for tissue engineering. chitosan was selected with benefit of high tissue compatibility attributed and wound healing through its activation of growth factors. And nonwoven chitosan fibrous matrix has well interconnected porosity. But chitosan itself has some of limitations in including rapid bone regeneration at initial states incorpor-ated of bioactive materials such as growth factors and ECM molecules. (omitted)
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Excipients of the drug products can sometimes affect the rate and extent of drug absorption. The changes in components or composition of them can also affect the pharmacological activity. So the quantity of excipients to be changed, the new excipients and atypically large amount of commonly used excipients should be considered as bioequivalence studies. (omitted)
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For the purpose of obtaining high bone forming efficacy, chitosan microgranules were developed as bone substitutes. Chitosan has been applied to conduct the extracellular matrix (ECM) formation in tissue regenerative therapy. Microgranules designed in this study confer drug releasingcapacity in bone defect over long period to enhance bone regeneration. (omitted)
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Jeong, Ji-Hoon;Park, Joon-Hong;Choi, Tae-Sik;Lee, Dong-Kyu;Jung, Chan-Heon;Son, Byung-Hyuk;Sohn, Uy-Dong 304.1
We aimed at determining bioavailability of tolperisone, a muscle relaxant. and developing a simple analysis in human blood using HPLC. A rapid and snsitive HPLC method was developed and validated using reverse-phase C18 column with retention time and limit of quantification of toferisone being 7.3 min and 20 ng/$m\ell$ , respectively. Quantification was performed at 260 nm with chlorphenesin as internal standard. (omitted) -
A simple and rapid method for the determination of theophylline (THP) in human serum was developed by a high performance liquid chromatography/UV detector and applied to pharmacokinetic study of THP in human volunteers.
${\beta}$ -Hydroxyethyltheophylline as internal standard was added to 200${\mu}\ell$ of human serum and the mixture was centrifuged at 13000 rpm for 10 min. (omitted) -
A simple, specific and sensitive method for the determination of levofloaxcin (LFX) in human serum was developed by a high performance liquid chromatography/diode array detector and applied to pharmacokinetic study of LFX in human volunteers. This method involves several steps such as precipitation with acetonitrile, extraction with methylene chloride, evaporation, and concentration, using 0.5ml of the serum. (omitted)
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Jeong, Ji-Hoon;Park, Joon-Hong;Choi, Tae-Sik;Lee, Dong-Kyu;Kang, Hee-Yun;Son, Byung-Hyuk;Sohn, Uy-Dong 305.2
We aimed at determining bioavailability of chlorphenesin carbamate, a muscle relaxant, and developing a simple analysis in human blood using HPLC. A rapid and sensitive HPLC method was developed and validated using reverse-phase C 18 column with retention time and limit of quantification of toferisone being 8.6 min and 0.5 ng/$m\ell$ , respectively. Quantification was performed at 260 nm with tolferison as internal standard. (omitted) -
The purpose of this study was to investigate the effect of ketoconazole(20mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel(40mg/kg) orally coadministered in rats. The plasma concentration of paclitaxel in combination with ketoconazole was increased significantly (coadministration p<0.05, pretreatment p<0.01) compared to that of control. (omitted)
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The purpose of this study was to investigate the effect of verapamil (5, 10, 20 mg/kg) on the pharmacokinetic parameters and the bioavailability of paclitaxel (50 mg/kg) orally coadministered in rats. The plasma concentration of paclitaxel with verapamil increased dose-dependently, and increased significantly in both coadministration (p<0.05) and pretreatment group (p<0.01) compared to that of control. (omitted)
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Metfotrmin is a biguanide antihyperglycemic agent often used for the treatment of non-insulin dependent diabetics(NIDDM). Metformin lowers both fasting and postprandial plasma glucose concentrations by improving insulin sensitivity at hepatic and peripheral tissues. The pharmacokinetics and pharmacodynamics of metformin were studied in Korean healthy volunteers at fasting state over 10 hours. (omitted)
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Lee, Jun-Woo;Kim, Sung-Chull;Yoo, An-Na;Chang, Hyun-Sung;Lee, Kyung-Hee;Park, Jong-Min;Nam, Doo-Hyun 307.2
The bioequivalence of two 12.72 mg domperidone maleate tablets (Sinil “perinal$\^$ ⓡ/” tablets vs. Janssen Korea “Motirium-M$\^$ ⓡ/” tablets) was assessed in healthy volunteers after oral administration of two tablets in a randomized crossover study. Blood samples were collected at specified time intervals, and plasma was analyzed for domperidone base using a validated HPLC method. (omitted) -
Sohn, Soo-Jung;Choi, Hong-Serck;Ahn, Mee-Ryung;Chung, Hye-Joo;Yoo, Tae-Moo;Lee, Min-Ho;Park, Moon-Seung;Shin, In-Chul;Kim, Ju-ll 308.1
We underwent this study to know correlation between the amount of portosysternic shunt/hepatic fibrosis and bioavailability parameters such as AUC, Cmax, Tmax and t1 /2 of high extraction ratio drug, propranolol, in CCl4-induced liver cirrhosis model of rats. This study describes the bioavaility study of propranolol(5 mg/kg), Shunt Index using thallium-201 per rectum scintigraphy to to measure the amount of portosystemic shunt indirectly and intrahepatic hydroxyproline content performed in the CCl4-induced liver cirrhosis model of rats. (omitted) -
In rats with water deprivation for 72 h (rats with dehydration), hepatic cytochrome P450 2E1 (CYP2E1) was 3-fold induced with an increase in mRNA, and glucose supplementation instead of food during 72-h water deprivation inhibited the CYP2E1 induction. Chlorzoxazone (CZX) is metabolized to 6-hydroxychlorzoxazone (OH-CZX) mainly by CYP2E1 in rats. (omitted)
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The purposes of this study were to evaluate bioequivalence (BE) using In-transformed pharmacokinetic parameters obtained from two risperidone products and to develop the analytical methods for the quantitative determination of risperidone in human serum. In addition, the in vitro dissolution profiles of the two risperidone products in various dissolution media: pH 1.2, 4.0, 6.8 and water (KP VII Apparatus II method) were assesed. (omitted)
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The pharmacokinetics and pharmacodynamics of torasemide were evaluated after an intravenous administration of the same total dose of torasemide at a dose of 1 mg/kg to rabbits with different infusion times, 1 min (treatment I), 30 min (treatment II), and 2 h (treatment III). The loss of water and electrolytes in urine induced by torasemide was immediately replaced with infusion of equal volume of lactated Ringer…s solution. (omitted)
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SD-2007 ia an apicidin analogue, possessing a potent histone deacetylase inhibiting activity. A rapid and senstive LC/MS method was developed for the determination of SD-2007 and its major active metabolite. apicidin. in rat serum. SD-2007 and apicidin was extracted by liquid-liquid extraction using methyl t-butyl ether. SD-2007 and apicidin were monitored in a SIM mode at m/z of 679 and 622, respectively. (omitted)
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The effects of differences in the rate and composition of intravenous fluid replacement for urine loss on the pharmacokinetics and pharmacodynamics of torasemide were evaluated using rabbits as the animal model. Each rabbit received 2-h constant intravenous infusion of 1 mg/kg ∼ 1 of torasemide with 0% replacement (treatment I, n = 6), 50% replacement (treatment II, n = 9), and 100% replacement with lactated Ringer's solution (treatment III, n = 8) as well as with 100% replacement with 5% dextrose in water(D-5-W, treatment IV, n=6). (omitted)
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Yu, Su-Yeon;Shin, Jee-Hyun;Bae, Soo-Kyung;Kim, Eun-Jung;Kim, Yoon-Gyoon;Kim, Sun-Ok;Lee, Dong-Ha;Lim, Hong;Lee, Myung-Gull 311.1
Dose-independent pharmacokinetic parameters of KR-60436, a new proton pump inhibitor, were evaluated after an intravenous, iv (5, 10, and 20 mg/kg) and an oral (20, 50, and 100 mg/kg) administration to rats. The hepatic, gastric, and intestinal first-pass effects were also measured after iv, intraportal (ip), intragastric (ig), and intraduodenal (id) administration at a dose of 20 mg/kg to rats. (omitted) -
The purposes of this study were to evaluate bioequivalence (BE) using In-transformed pharmacokinetic parameters obtained from two fluconazole products and to develop the analytical methods for the quantitative determination of fluconazole in human serum. In addition, the in vitro dissolution profiles of the two fluconazole products at dissolution media: 0.1 M hydrochloride (KP Ⅶ Apparatus II method) were assessed. (omitted)
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Kim, Jeong-Hoon;Jang, Sun-Woo;Bac, Woong-Tak;Kweon, Jong-Weon;Kim, Won-Bac;Yoon, Mi-Kyeong;Choi, Young-Wook 312.1
Silybin is the main component of Cardus marianus extracts (Silymarin) originated from Silybum marianum, called as milk thistle. It has a hepato-protective effect and is used clinically for the treatment of liver disease. But it is water-insoluble and is poorly absorbed from the gastrointestinal tract, resulting in very low oral bioavailability. Polymeric mixed-micelle precursor formulation containing surfactants, co-solvents, and block-co polymers with Cardus marianus extracts was made to enhance the dissolution rate of silybin and encapsulated with soft gelatin capsule. (omitted) -
Lee, Mi-Hye;Lee, Dae-Young;Bae, Soo-Kyung;Kim, Eun-Jung;Kim, Yoon-Gyoon;Kim, Sun-Ok;Lee, Dong-Ha;Lim, Hong;Yoo, Sung-Eun 312.2
The purpose of this study was to report dose-independent pharmacokinetics of KR-31543, a new neuroprotective agent for ischemia-reperfusion damage, after intravenous and oral administration and first-pass effects after intravenous. intraportal, intragastric, and intraduodenal administration in rats. After intravenous (10, 20 and 50 mg/kg) and oral (10, 20 and 50 mg/kg) administration, the pharmacokinetic parameters of KR-31543 were dose-independent. (omitted) -
DA-125, a novel anthracycline analog containing fluorine with decreased cardiotoxicity and increased antitumor activity of adriamycin (ADM), developed by Research Laboratories of Dong-A Pharmaceutical. DA-125, water soluble prodrug of M1, is a
${\beta}$ -alanine derivative of M1 (FT-ADM). DA-125 was rapidly hydrolyzed to M1, and M1 was metabolized to both M2 and M3. (omitted) -
This study was conducted to investigate the pharmacokinetic characteristics of a synthetic opioid, Tridol\ulcornerCapsule (tramadol hydrochloride from Yuhan Pharmaceutical Co., Ltd., Korea) in 24 healthy Korean volunteers after a single dose administration. The volunteers received two capsules of 50 mg dose. Plasma samples were obtained over a 24-hour interval, and tramadol concentrations were obtained over a 24-hour intervalm and tramadol concentrations were determined by validated HPLC methods with a fluorescence detector. (omitted)
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Examination was made of the urinary metabolite(s) of CKD-712, which is a chiral compound, named S-YS49 derived from higenamine (one component of Aconite spp.) derivatives. First of all. to analyze the metabolite(s) of CKD-712, a simple and sensitive detection method for CKD-712 was developed by using gas chromatography-mass spectrometry(GC/MS). (omitted)
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Jean, Hee-Kyung;Choi, Hae-Yeon;Kim, Youn-Jung;Kim, Young-Soo;Kim, Young-Soo;Kim, Mi-Kyung;Lee, Seung-Ho;Jung, Sang-Hun 314.2
Sophoricoside was isolated as the inhibitor of IL-5 bioactivity from Sophora japonica (Leguminosae). To develope as novel anti-allergic drug. kinetic study was performed in rats. Serum concentration of sophoricoside was measured by gas chromatography-mass spectrometry (GC/MS) in male Sprague-Dawley rat (250${\pm}$ 10g, n=5) after oral administration of sophoricoside (100mg/kg). (omitted) -
Yoon, Kyung-Eun;Chung, Soo-Youn;Park, Ki-Sook;Choi, Hong-Suk;Baek, Min-Sun;Jung, Sung-Hee;Choi, Sun-Ok 315.1
After beginning the new medical system separating the prescription from the drug dispensary, the demand of bioequivalence test significantly increases to show the equivalence between the test and reference drugs as a result of amendment of the pharmaceutical affairs law which allows a generic substitution. Accordingly the standard protocols provided by the government are required for reducing the period andthe cost to perform the bioequivalence study. (omitted) -
Polyethylenimine (PEI) has been used as a non-viral gene delivery carrier. To improve the efficacy of transfection, transferrin was incorporated by covalent linkage to PEI. As a model plasmid DNA, pHME185/b-gal, a mammalian expression vector was used. The transferrin-polyethylenimine (TfPEI) was synthesized by conjugate PEI with transferrin using sodium periodateand and characterized by FT-IR and 1H-NMR. (omitted)
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N-acetylneuraminic acid is one of the major derivatives of sialic acid. is widely distributed in mammalian cells as the
${\alpha}$ 2-3- or${\alpha}$ 2-6-linked nonreducing terminal residue of oligosaccharide chains of glycoconjugates, and plays important structural and functional roles at the cell membrane surface. The analysis of sialylated glycoproteins is an important part of glycoprotein characterization, especially because sialylation or desialylation in oligosaccharides often causes dramatic changes in the function of glycoproteins. (omitted) -
Immunoglobulin Y (IgY) obtained from chicken as the immunization host brings several advantages to antibody production, such as improved yield, lower cost, longer stability, and higher specificity than mammalian immunoglobulin. In the present study, we attempted to purify Maackia fauriei lectin using antilectin IgY-affinity chromatography in order to produce a good yield and to reduce the purification time. (omitted)
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Carbohydrate-binding proteins have been isolated from various sources, including plants, animals, fungi, and bacteria, and they have been used extensively in the detection, localization, and isolation of glycoconjugates. Many carbohydrate-binding proteins are purified from mushrooms, however, only a few proteins with sialic acid-binding specificity have been reported. In the present study, a novel sialic acid-binding protein, designated PJA, has been purified from the mushroom Paecilomyces japonica. followed by extraction and affinity chromatography. (omitted)
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The current study was performed to observe the effect of Sun Ginseng (SG) on hemodynamics such as blood flow rate (BF), blood flow velocity (BV), heart rate (HR), systolic blood pressure (SBP) and diastolic blood pressure (DBP), and body temperature (BT) in healthy young men. This is a randomized, single-blind study observed during 6 hrs after orally single administration of SG. (omitted)