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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Biomolecules and Therapeutics
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Journal DOI :
The Korean Society of Applied Pharmacology
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Volume & Issues
Volume 12, Issue 4 - Dec 2004
Volume 12, Issue 3 - Sep 2004
Volume 12, Issue 2 - Jun 2004
Volume 12, Issue 1 - Mar 2004
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Effect of Erythromycin on Basal and Stimulated Mucin Release from Cultured Hamster Tracheal Surface Epthelial Cells
Park, Ji-Sun ; Seok, Jeong-Ho ; Hur, Gang-Min ; Lee, Jae-Heun ; Park, Kyeung-A ; Lee, Choong-Jae ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 57~61
In the present study, we investigated whether lipopolysaccharide induce mucin release and erythro-mycin affect basal and adenosine triphosphate-induced (stimulated mucin release, from airway goblet cells. Confluent primary hamster tracheal surface epithelial cells were metabolically radiolabeled and chased for 30 min or 24 hr in the presence of varying concentrations of lipopolysaccharide or erythromycin to assess the effects on
-mucin release. The results were as follows : 1) Lipopolysaccharide failed to induce mucin release, 2) Erythromycin showed no effect on both basal and stimulated mucin release during 30 min of 24 hr treatment period. We conclude that lipopolysaccharide and erythromycin can not affect mucin release by direct acting on airway mucin-secreting cells.
Hepatic Vascular Stress Gene Expression in the Liver Response to Trauma
Lee, Sun-Mee ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 62~67
Trauma remains one of the important sources leading to systemic inflammatory response anti sub-sequent multiple organ failure. Although hepatic microvascular dysfunction occurs during trauma, the mechanism responsible remains unclear. The aim of this study was to investigate the effect of trauma on hepatic vascular stress gene expression. Femur fracture (EFx) was induced by torsion to the femur at midshaft. Liver samples were taken for RT-PCR analysis of mRNA for gtenes of interest: endothelin-1 (ET-1), its receptors
, nitric oxide synthases (iNOS and eNOS), cyclooxygenase-2 (COX-2), heme oxygenase-1 (HO-1), and tumor necrosis tactor-
). The expression of ET-1 mRNA was significantly increased by FFx. Expression of mRNA in FFx group showed no change in
, iNOS and HO-1 and showed a slight increase of 2.2-fold and 2.7-fold for eNOS tll1d COX-2, respectively. The level of TNF-
mRNA significantly increased in FFx group. In conclusion, mild trauma alone causes little change in expression of vasoactive mediators.
The Regulatory Mechanism of Cerebral Blood How of Adenosine A
Receptor Agonist in the Rats
Kang, Hyung-Kil ; Shin, In-Chul ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 68~73
This study was performed to investigate the regulatory mechanism of cerebral blood How of adenosine
receptor agonist in the rats, and to define whether its mechanism is mediated by nitric oxide (NO), adenylate cyclase and guanylate cyclase. In pentobarbital-anesthetized, pancuronium-paralyzed and artificially ventilated male Sprague-Dawley rats, all drugs were applied topically to the cerebral cortex. Blood flow from cerebal cortex was measured using laser-Doppler flowmetry. Topical application of an adenosine
receptor agonist [5'-(N-cyclopropyl)-carboxamidoadenosine (CPCA; 4 umol/l)] increased cerebral blood flow. This effect of CPCA (4 umol/l) was blocked by pretreatment with NO synthase inhibitor [
-nitro-L-argine methylester (L-NAME; 140 umol/l)] and adenylate cyclase inhibitor [MDL-12,330 (20 umol/l)]. But the effect of CPCA (4 umol/l) was not blocked by pretreatment with guanylate cyclase inhibitor [LY-83,583 (10 umol/l)]. These results suggest that adenosine
receptor increases cerebral blood How. It seems that this action of adenosine
receptor is mediated via the NO and the activation of adenylate cyclase in the cerebral cortex of the rats.
Inhibition of GLUT-1 Expressed in Xenopus laevis Oocytes by Acetoxyscirpendiol of Paecilomyces tenuipes
Lee, Dong-Hee ; Kim, Ha-Won ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 74~78
Paecilomyces tenuipes, a caterpillar fungus, contains many health-promoting ingredients. Recent reports indicate that consumption of P. tenuipes helps reducing blood sugar content for diabetes. Mechanism for reduction in the circulatory sugar content, however, still remains least understood. Methanolic extraction of P. tenuipes (MPT) was prepared and acetoxyscirpendiol (ASD) was subsequently purified limn MPT. Glucose transporter-1 (GLUT-1) was expressed in the Xenopus oocytes and the effect of MPT or ASD on the expressed GLUT-1 was analyzed according to the uptake of 2-dideoxy-D-glucose (2-DOG). MPT was shown to inhibit GLUT-1 activity significant1y compared to the non-treated control. In the presence of ASD and its derivatives, GLUT-1 activity was greatly inhibited in a dose-dependent manner. Among ASD and its derivatives, AS-1 showed most significant inhibition. Taken together, these results strongly indicate that ASD in P. tenuipes may serve as a functional substance in lowering blood sugar in the circulatory system. ASD and its derivatives can be utilized as inhibitors of GLUT-1.
Regulatory Effect of Th-2 Cytokine Production in Mast Cells by 02PS15
Na, Ho-Jeong ; Seo, Young-Wan ; Lee, Eun-Hee ; Kim, Hyung-Min ; Hong, Seung-Heon ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 79~84
02PS15 extracts (BuOH,
, and crude extracts) significantly inhibited IL-4 and IL-6 secretion from the phytohemagglutinin (PHA)-plus phorbol 12-myristate 13-acetate (PMA)-induced peripheral blood mononuclear cleas (P<0.05). 02PS15 extracts (BuOH and crude extracts) also significantly inhibited the histamine release from rat peritoneal mast cells (P<0.05). Significant reduced levels (P<0.05) of PMA- and A23187-induced IL-8 were observed in the human mast cell line, HMC-1, with O2PS15 extracts (BuOH and crude extracts). 02PS15 extracts (BuOH and crude extract) downregulated the expression of IL-6 and IL-8 in the activated HMC-1. These results suggest that O2PS15 has the inhibitory effect of atopic allergic reaction anil this might be useful for clinical application to treat several allergic diseases such as atopic dermatitis.
Inhibition of Apoptosis is Responsible for the Acquired Resistance of K562 Cells to Cisplatin
Lee, Soo-Yong ; Kim, Dong-Hyun ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 85~91
In all attempt to elucidate the role of apoptosis in drug resistance, cisplatin-resistant human chronic myelogenous leukemia (CML) K562 cells (K562/CDDP) were established and compared with drug sensitive parent cells (K562) in the induction of apoptosis. K562/CDDP cells were 5-fold more resistant to cisplatin compared to K562 cells. In addition, K562/CDDP cells were significantly more resistant to apoptois as judged by DNA fragmentation and DAPI staining. K562/CDDP cells exhibited decreased proleolytic activity of caspase-3 and this was further demonstrated by decreased cleavage of its substrate poly (ADP-ribose) polymerase (PARR- Western blot analysis showed that K562/CDDP cells had longer sustained levels of BCL-
whereas no difference was noted in the level of Bcl-2. the translocation of Bax to mitochondria was significantly delayed in K562/CDDP cells. These results suggest that the reduced translocation of Bax and the sustained expression of BCL-
may cause resistance to apoptosis through prevention of mitochondria release of cytochrome c, which subsequently induces reduction of caspase-3 activity and that this response is partly responsible for the acquired resistance to cisplatin ill K562 cells.
Effect of Depletion and Oxidation of Cellular GSH on Cytotoxicity of Mitomycin Small Cell Lung Cancer Cells
Lee, Chung-Soo ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 92~100
Effect of the depletion or oxidation of GSH on mitomycin c (MMC)-induced mitochondrial damage and cell death was assessed in small cell lung cancer (SCLC) cells. MMC induced cell death and the decrease in the GSH contents in SCLC cells, which were inhibited by z-LEHD.fmk (a cell permeable inhibitor of caspase-9), z-DQMD.fmk (a cell permeable inhibitor of caspase-3) and thiol compound, N-acetylcysteine. MMC caused nuclear damage, release of cytochrome c and activation of caspase-3, which were reduced by N-acetylcysteine. The depletion of GSH due to L-butionine-sulfoximine enhanced the MMC-induced cell death and formation of reactive oxygen species in SCLC cells, whereas the oxidation of GSH due to diamide or
did not affect cytotoxicity of MMC. The results show that MMC may cause cell death in SCLC cells by inducing mitochondrial dysfunction, leading to activation of caspase-9 and -3. The MMC-induced change in the mitochondrial membrane permeability, followed by cell death, in SCLC cells may be significantly enhanced by the depletion of GSH. In contrast, the oxidation of GSH may not affect cytotoxicity of MMC.
Behavioral Sensitization and M1 Muscarinic Acetylcholine Receptor mRNA Expression in Methamphetamine-Administered Mice
Kim, Kyung-In ; Cho, Jae-Han ; Park, Hyun-Jung ; Lee, Seok-Yong ; Jang, Choon-Gon ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 101~107
Repeated administration of psychostimulants such as amphetamines increases locomotor activity in rodents. These drugs, including methamphetamine, enhance dopaminergic neurotransmission and result in hyper-locomotion and behavioral sensitization. It is well known that the existence of a complex balance between the cholinergic and dopaminergic systems in the central nervous system. Thus, behavioral sensitization by methamphetamine may be related to the expression of the M1 muscarinic acetylcholine receptors gene. The present study investigated the changes of M1R mRNA in hyperlocomotor activity and behavioral sensitization by methamphetamine (2 mg/kg) in mice. Our results showed that M1R mRNA expression was increased in the frontal cortex and the hippocampus region (the CA2 region) in the acute methamphetamine administered group compared to the saline administered group. In the chronic group, M1R mRNA expression was increased in the frontal cortex ill1d the hippocampus regions (CA2 and DG regions) in melt1amphetamine administered group compared to saline control group. These results indicate that acute or chronic treatment of mathamphetamine leads to the region-specific changes in mRNA expression levels of M1R. Therefore, Therefore, the present result suggests that M1R may play a role in modulating of methamphetamine-induced behavioral sensitization in mice.
Effects of Cyclic Nucleotides on the Cerebral Blood Row Response Induced by Adenosine A
Receptor Agonist in the Rats
Kim, Hyun-Seung ; Shin, In-Chul ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 108~113
This study was performed to investigate the regulatory mechanism of cerebral blood flow of adenosine
receptor agonist in the rats, and to define whether its mechanism is mediated by adenylate cyclase and guanylate cyclase. in pentobarbital-anesthetized, pentobrabital-paralyzed and artificially ventilated male Sprague-Dawley rats, all drugs were applied topically to the cerebral cortex. Blood How from cerebral cortex was measured using laser-Doppler flowmetry. Topical application of an adenosine
receptor agonist, 5'-N-ethylcar-boxamidoadenosine (NECA; 4 umol/l) increased cerebral blood flow. This effect of NECA (4 umol/l) was not blocked by pretreatment with adenylate cyclase inhibitor, MDL-12330 (20 umol/l). But effect of NECA (4 umol/l) was blocked by pretreatment with guanylate cyclase inhibitor, LY-83383 (10 umol/l). These results suggest that adenosine
receptor increases cerebral blood flow. It seems that this action of adenosine
receptor is mediated via the activation of guanylate cyclase in the cerebral cortex of the rats.
General Pharmacological Study of CJ-11828, an Amlodipine adipate
Choi, Jae-Mook ; Lee, Sung-Hak ; Kim, Il-Hwan ; Park, Jie-Eun ; Park, Choong-Sil ; Youn, Yong-Sik ; Lim, Dong-Kwon ; Cho, Sung-Hwan ; Chang, Jun-Hwan ; Do, Sun-Hee ; Kim, Eun-Joo ; Kim, Young-Hoon ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 114~121
This study was undertaken to evaluate the general pharmacological properties of CJ-11828, an amlodipine adipate, in experimental animals and in vitro system. CJ-11828 had no effects on general behavior, motor coordination, writhing syndromes, pentetrazol-induced chemoshock and electric shock in mice at dose levels of 3,10, anti 30 mg/kg, po. But there were decrease of body temperature, prolongation of sleeping time, and inhibition of intestinal activity in mice treated with CJ-11828 at doses of 10 and 30 mg/kg, po. CJ-11828 decreased the blood pressure in coscuous fog at the dose level of 2mg/kg, po, but it was expected as a result of pharmacological activity of CJ-11828. Any effect on respiratory system was not observed in conscious rat at doses of 3,10, and 30 mg/kg, po. The slight decrease in spontaneous motor activity was observed in mice treated with CJ-11828 at high dose, 30 mg/kg. In vitro experiments, CJ-11828 had no effect on agonists-induced contraction of isolated guinea pig ileum at 0.1, 1, and 10
M. Based on these results, it was concluded that CJ-11828 had no pharmacological effect ill these studies even up to the 36-fold anticipated clinical dose, 3 mg/kg.
Evaluation of Cancer Chemopreventive Potential of Various Grape Shoot Extracts and Refined Materials Using in vitro Bioassay Systems
Min, Hye-Young ; Hong, Ji-Young ; Kim, Moon-Sun ; Chung, Hwa-Jin ; Cho, Yong-Jin ; Lee, Sang-Kook ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 122~128
Since reactive oxygen species, prostaglandins, and nitric oxide are closely involved in various pathological conditions anti play important roles in the initiation, promotion, and progression of carcinogenesis, agents that modulate the production or activity of them might be considered as cancer chemopreventive agents. In the present study, we evaluated chemopreventive potential of some grape shoot extracts and their refined materials using various in vitro assay systems. As a result, both grape shoot extracts and refined materials possessed effective radical scavenging activities about 70~80% at the concentration of 500
g/ml, and especially the Sheridan shoot extract showed the most potent 1, 1-diphenyl-2-picrylhydrazyl radical scavenging activity that was similar to resveratrol. In addition, refined materials from grape shoot extracts suppressed lipopolysaccharide-induced nitric oxide production in macrophage cells, anti refined materials from Kyoho and Campbell shoot extracts exhibited similar inhibitory activities with
value of 224
g/ml and 285
g/ml, respectively. In addition, at the concentration of 50
g/ml, all of refined materials inhibited cell proliferation against various human cancer cells about 30~40% compared to control. These findings suggest that grape shoot extract and their refined materials might be useful sources for the development of chemopreventive agents and/or functional foods.
Effect of Hwangryunhaedoktang on Contact Hypersensitivity and Passive Cutaneous Hypersensitivity in Mice
Lee, Kun-Ho ; Shin, Young-Wook ; Kim, Dong-Hyung ;
Biomolecules and Therapeutics, volume 12, issue 2, 2004, Pages 129~132
During the screening program to discover antiatopic agents from herbal formulas, we investigated the inhibitory effect of Hwangryunhaedoktang (HT) on passive cutaneous anaphylaxis and oxazolone-induced mouse ear dermatitis. HT significantly inhibited PCA reaction in mice at doses of 50 and 200 mg/kg with inhibitory activity of 31 and 53%, respectively. HT at concentration of 0.05 and 0.1% inhibited ear swelling by 23 and 46% at 16 days in oxazolone-induced mouse ear dermatitis. Both HT with anti without human intestinal microflora showed potent inhibitory activity on the
-hexosaminidase release induced by IgE. Based on these findings, HT may be a usable agent for skin disorder contact dermatitis.