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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Biomolecules and Therapeutics
Journal Basic Information
Journal DOI :
The Korean Society of Applied Pharmacology
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Volume & Issues
Volume 8, Issue 4 - Dec 2000
Volume 8, Issue 3 - Sep 2000
Volume 8, Issue 2 - Jun 2000
Volume 8, Issue 1 - Mar 2000
Selecting the target year
The Anti-inflammatory and Analgesic Actions of the Root of Pulsatilla koreana
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 207~212
The root extract of pulsatilla koreana has been used as antibacterial, antiparasitic and anti-inflam-matory analgesic agents in Traditional Medicine in Korea. Thus anti-inflammatory and analgesic actions of the methanol and water extracts of the root were investigated by administration in oral and intravenous route. From the results, it is concluded that the extracts exhibited the potent anti-inflammatory and analgesic actions in intravenous administration, but did not show the actions in oral administration in animals.
Leucostim, A Human Granulocyte-Colony Stimulating Factor, Facilitates Granulopoiesis After Bone Marrow Transplantation In Mice
Ahn, Byoung-Ok ; Kang, Soo-Hyoung ; Kim, Won-Bae ;
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 213~216
In vivo administration of Leucostim, a human recombinant granulocyte colony-stimulating factor (G-CSF), was evaluated for the effects on survival, hematologic recovery, and colony forming unit- spleen (CFU-5) in murine bone marrow transplantation (BMT) model. Sublethally irradiated (9 Gy) mice received bone marrow cells from untreated mice, and then were treated with G-CSF subcutaneously at doses of 2.5,5, or
/kg or vehicle solution (control) for 14 days from one day after BMT. There was no effect of irradiation and BMT on mortality. The repeated subcutaneous injections of Leucostim for 14 days post- BMT significantly facilitated hematologic recovery compared with vehicle control in a dose-dependent manner. Moreover, mice treated with Leucostim had significantly increased numbers of CFU-s colonies on day 10 post-BMT. These results suggest that Leucostim, a new G-CSF, has beneficial effects on hematologic reconstitution after BMT.
Induction of Secretory and Cellular Activities by Pneumococcal Teichoicated Fragments in Macrophages
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 217~222
Bacterial components and their derivatives have been reported to mediate various immunomodulating activities and to activate immune cells including macrophage. In this study, the secretory and cellular macrophage response to teichoicated fragments (TFs) from pneumococcal cell wall subcomponent were examined. Tumoricidal activity was measured by MTT assay and secretory molecules were assessed by biological assay. After stimulation of macrophages with various doses of TFs for 18hrs, secretion of TNF-
, nitrite and
were significantly increased as compared to medium-treated control. In addition, tumorcidal activity of TFs-treated macrophages was enhanced, whereas production of IL-1 and IL-6, and phagocytic activity were not induced. These data suggest that TFs is a potent inducer of macrophage secretory and cellular activities.
The effect of Propolis on Endotoxin-induced thrombosis
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 223~227
Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used for traditional medicines as early as 300 B .C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. To investigate activities of chrysin, one of propolis effective compounds for blood coagulation system was injected endotoxin (4000 EU/kg, i.v.) in rats at 1 hr after administered chrysin (20 mg/kg, p.o.). This study was resulted that chrysin has antiplatelet aggregation activity in vitro, delay of blood clotting time and prothrombin time, and reduction of fibrinogen and FDP in vivo. Chrysin has increased SOD activity, GSH content and GST activity, and decreased MDA content in liver. The result suggests that the antithrombosis effect of chrysin is suppressive activity for a blood coagulation system and antioxidative activity.
In Vitro Cytotoxicity of a Novel Platinum(II) Coordination Complex Containing Diaminocyclohexane
Jung, Jee-Chang ; Kim, Soon-Ae ; Kim, Young-Kyu ; Chang, Sung-Goo ; Rho, Young-Soo ;
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 228~234
We have synthesized a novel platinum(II) coordination complex containing trans-ι-1,2-diaminocy-clohexane (DACH) as a carrier ligand and 1,2-dichloroethane (DCE) as a leaving group. A new series of [Pt(trans-ι-DACH)(DCE)](PC) was evaluated for its cytotoxic activity on MKN-45 human gastric adenocar-cinoma cells and normal primary cultured kidney cells. The new platinum complex has demonstrated high efficacy in the cytotoxicity against MKN-45/P, MKN-45/ADM and MKN-45/CDDP cell-lines. The cytotoxicity of PC against rabbit proximal renal tubular cells, human renal cortical cells and human renal cortical tissues, determined by MTT assay, the [
]-thymidine uptake arid glucose consumption tests, was found to be quite less than those of cisplatin. Based on these results, this novel platinum(II) coordination complex appears to be better for improving antitumor activities with low nephrotoxicity and is a valuable lead in the development of new, clinically available anticancer chemotherapeutic agents.
Antitumor Activity of the Intergeneric Protoplast Fusant between Lentinus edodes and Coriolus versicolor
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 235~240
Antitumor effect of LC43, a protein-bound ploysaccharide (M.W. 43 kDa) that was purified from intergeneric protoplast fusant of Lentinus edodes and Coriolus versicolor, was elucidated against mouse sarcoma 180 cell in vitro and in vivo. By injecting LC43 into ICR mice bearing solid or ascitic sarcoma 180, tumor regression and survival rates were investigated. To examine the effects of LC43 on immunopotentiation activity. immunoorgan weight, B cell differentiation, T cell activity and macrophage activation were determined. LC43 showed antitumor effects against both solid tumor and ascitic tumor of sarcoma 180. It did not change significantly the immunoorgan weight but potentiated immune responses such as B cell differentiation and the release of superoxide anion from macrophages. These results suggest that the protein-bound polysaccharide of LC43 exhibited antitumor activities through the activation of immune-related cells and acted as an immunmodulator.
Effects of Selective Thromboxane
-Receptor Antagonist, KT2-962 on Adriamycin-induced Nephrotoxicity in Rats
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 241~247
The present study was designed to assess the protective effect of a selective thromboxane
receptor antagonist, KT2-962 (KT2) and possible mechanisms of adriamycin(AD)-induced nephrotoxicity in rats. The male Wistar rats were given either of AD (7.5 mg/kg, i.v.) alone in the AD-group (n=5) or in KT2+AD- group (n=5) which is a combination of AD and KT2 (30 mg/kg/day, i.p.) for 10 days from 3 days before and 7 days after AD injection. The body weight, 24-hours urine volume, urine protein and urinary N-acetyl-
-D-glu-cosaminidase (NAG) activity were measured with an interval of 2 days during 1 week. BUN, serum creatinine and creatinine clearance were measured on the 7th day. KT2 has significantly suppressed AD-induced change of body weight, 24-hours urine volume, urine protein and urinary NAG activity in the KT2+AD-group. The change of BUN, serum creatinine and creatinine clearance were significantly inhibited in the B7T2+AD-group. Based on these results, it is concluded that KT2 prevents AD-induced nephrotoxicity and suggests that endogenous thromboxane A2 may play an important role in AD-induced nephrotoxicity in rats.
Mutagenicity Study of (R)-JG-381, A New Antidiabetic Agent
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 248~254
(R)-JG-381, a R form of alkylglycidic acid derivative, was examined for mutagenicity in the reverse mutation test on bacteria, chromosomal aberration test on cultured mammalian cells and micronucleus test in mice. In the reverse mutation test on bacteria using Salmonella typhimurium strain TA98, TA100, TA102, TA1535, TA1537 with or without a metabolic activation system (S9 mix), (R)-JG-381 did not affect the revertant colonies but significantly increased revertant colonies in one test strain, TA98, compared with the vehicle control. In the chromosomal aberration (CA) test using cultured Chinese Hamster Lung fibroblast(CHL) cells, the number of aberrant cells was clot increased in the presence or absence of 59 mix at concentration of the (R)-JG-381 0.025
l/m1 to 0.1
l/m1, compared with vehicle control. In the micronucleus (MN) test, micronucleated polychromatic erythrocytes in the (R)-JG-381-treated mice were not different from those of the vehicle-treated mice.
The comparison of histological effects of musk containing and civet containing WooHwangChungSimWon on the cerebral ischemia
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 255~261
WooHwangChungSimWon is a traditional prescription for treating with hypertension, arteriosclerosis, coma, and stroke in China, Korea, and Japan. In the new presciption of WooHwangChungSimWon, the covet is substituted for the musk, the major component of WooHwangChungSimwon, because of the prohibition law about the musk. We have made a comparative study of the effects on the ischemic damage between the musk containing and civet containing WooHwangChungSimWon. In order to investigate the effects of WooHwangChungSimWon on the ischemic damage, each samples were administrated for 12 days, ischemia was induced for 10 minutes at 7th day, and immunohistochemistry was performed in the region of hippocampus of mongolian gerbils. According to the result of immunohistochemistry, the survival rates of neuroal cells in the hippocampal CA1 region are 37.8% in the high dose of musk containing WooHwangChungSimWon (HM-WHCSW) administrated group, 27.8% in low dose of civet containing WooHwangChungSimWon (LC-WHCSW), and 35.5% in high dose of civet containing WooHwangChungSimWon (HC-WHCSW) administrated group. These survial rates were significantly different from the survival rate of sham control group (14.4%). The results suggest that all the samples except the low dose of musk containing WooHwangChungSimWon (LM-WHCSW) have protective or preventive effects on cerebral ischemia.
Bioequivalence Evaluation of the Tiropramide hydrochloride
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 262~268
The bioequivalence of two tiropramide products was evaluated in 18 health male volunteers following oral administration. Test product was Tira
tablet (Shin Poong SP-102) (Shin Poong Pharm. Co., Ltd.) and reference product was Tirop
tablet (Dae Woong Pharm. Co., Ltd.) One capsule of the test and reference product containing 100 mg of tropramide.hydrochloride was administered to the volunteers by randomized two period cross-over study (2
2 Latin square method). The drug concentration in plasma was determined by GC/MS for over a period of 12hours after administration. Analysis of variance reveal that there are no differences in AUC (area under the plasma concentration-time curve from time zero to infinity), Cmax (maximum plasma concentration) and Tmax (time to reach Cmax). The differences of mean AUC, Cmax and Tmax between two products were 3.85, 1.47 and -3.6%, respectively. Minimum detectable differences (%) at
=0.1 were all less than 20% given as a guideline (18.07, 17.00 and 20.69% for AUC, Cmax and Tmax, respectively). From these results, the two products are bioequivalent.ent.
Clinical Pharmacokinetic Profiles of Hanmi SMEDDS Silymarin Soft Capsule Preparation
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 269~275
Silibinin(silybin) is the active component of silymarin from Silybum marianum and has hepato-protective effect. It is water-insoluble and has low bioavailability. To improve its bioavailability, self-micro-emulsifying drug delivery system (SMEDDS) has been developed by Hanmi Pharmaceutical Company (Silyma
140 soft capsule). In this study, the pharmacokinetic profiles of Silyma
were examined and compared it with a reference preparation, L Caps140 of B Pharmaceutical Company. This study was approved by Yonsei University Severance Hospital IRB(approval No. CR0004) and followed the bioequivalence test guideline of Korean FDA. Eighteen healthy adult volunteers were allocated based on 2
2 Latin square cross-over design. They were given 2 capsules (each contains silymarin 140 mg (60 mg as silibinin)) of either drug at each period and crossed over after a week of drug-free washout period. Blood concentration of silibinin was measured by HPLC. The
and AUC of the Silyma
402.7 ng/ml and 3323.3
824.7 ng.h/ml, respectively, and were significantly higher than those of reference preparation. The Tmax was 0.8
0.3 h and significantly shorter than reference preparation. The
2/ of both drugs were comparable. Percent differences in means against reference preparation were +88.3% for AUC, +222.6% for
, and -61.1% for
Molecular Interaction Between Interleukin-8 Receptor and G
16 subunit G protein
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 276~280
In order to identify the domains of the G
16 subunit G protein that are responsible for its activation by the Interleukin-8 receptor, a serious of chimeras between G
16 and G
11 were assessed for their abilities to be activated by these receptors. Co-expression of IL-8 receptor and chimeras in which the carboxyl-terminal regions of G
11 were replaced from 30 up to 156 amino acid residues with the corresponding regions of G
16 demonstrated that C-terminal 156 amino acid residues of the G
16 were not sufficient to confer IL-8 receptor interaction specificity. Testing of a reciprocal serious of chimeras composed of G
16 sequences at the amino terminus and G
11 sequences at the carboxyl terminals revealed that sequences extending from the amino tar- minus to amino acid 209 of G
16 were sufficient to 7ndow the chimera with 75-80% of interaction specificity for 7-8-induced activation. These results suggest th,.7t combined interactions of the C-terminal 30 amino acid residues and certain domains extending from the arts.ino terminus to amino acid 209 of Gal 6 protein may be involved in its couplings to IL-8 receptor.tain domains extending from the arts.ino terminus to amino acid 209 of Gal 6 protein may be involved in its couplings to IL-8 receptor.
Detection of Taurine in Basidiomycetes
Park, Tae-Sun ; Park, Jung-Eun ; Shim, Mi-Ja ; Kim, Byong-Kak ;
Biomolecules and Therapeutics, volume 8, issue 3, 2000, Pages 281~284
Taurine is one of the essential amino acids for humans and many of mammals. It is produced and contained in fleshes, shells, plants and algae, but has never been found in fungi. We examined six mushrooms for taurine and detected taurine in five of them. Taurine was determined by an automated amino acid analyzer using ion-exchange chromatography, being eluted between phosphoserine as a distinct peak on the chromatogram. Fruit bodies of Flammulina velutipes contained
moles/100g fresh wt. the highest level among them, Agaricus bisporos
moles, Lentinus edodes
moles, Pleurotus ostreatus
moles, and Auricularia auricula-judae
moles. Taurine was not detected in Ganoderma lucidum. As far as fungi are concerned, this is the first report of the detection of taurine in Basidiomyces.