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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
> Journal Vol & Issue
Biomolecules & Therapeutics
Journal Basic Information
Journal DOI :
The Korean Society of Applied Pharmacology
Editor in Chief :
Volume & Issues
Volume 9, Issue 4 - Dec 2001
Volume 9, Issue 3 - Sep 2001
Volume 9, Issue 2 - Jun 2001
Volume 9, Issue 1 - Mar 2001
Selecting the target year
SAR of COX-2 Inhibitors
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 69~78
Cyclooxygenase (COX) is an enzyme, which catalyzes the production of prostaglandins from arachi-donic acid and exists in two isoforms (COX-1 and COX-2). COX-1 is involved in the maintenance of physiological functions such as platelet aggregation, cytoprotection in the stomach and maintenance of normal kidney function. COX-2 is induced significantly in vivo under inflammatory conditions. COX-1 and COX-2 serve different physiological and pathological functions. All commercially available nonsteroidal antiinflammatory drugs (NSAIDS) are inhibitors of both COX-1 and COX-2. Therefore, selective inhibitors of COX-2 may be effective antiinflammatory agents without the ulcerogenic effects associated with current NSAms. Since the mid 1990s, a number of reports have been appeared on the preparation and biological activity of selective COX-2 inhibitors. Recently celecoxib, and rofecoxib, the representative COX-2 inhibitors, are introduced in the drug market. In this paper the relationship of structure-activity for selective COX-2 inhibitors is reviewed.
Cloning and Immunological Characterization of the 84-kDa Heat Shock Protein, ClpL, in Streptococcus pneumoniae
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 79~87
Heat shock proteins serve as chaperone by preventing the aggregation of denatured proteins and promote survival of pathogens in harsh environments. In this study, heat shock gene encoding a 84-kDa (p84) protein, which is one of the three major heat shock proteins in S. pneumoniae, was cloned and characterized. PCR with a forward primer derived from N-terminal amino acid sequence of the p84 and a reverse primer derived from the conserved second ATP-binding region of Clp family was used for amplification of the gene encoding the p84 and subsequently the PCR product was used for sequence determination. Sequence analysis of the p84 gene demonstrated that it is a member of ClpL. The deduced amino acid sequence of pneumococcal ClpL shows homology with other members of the Clp family, and particularly, even in variable leader region, with bovine Clp-like protein and L. lactis ClpL. S. pneumoniae clpL is the smallest clop member (701 amono acids) containing the two conserved ATP-binding regions, and hydrophilic N-terminal variable region of pneu-mococcal Clp ATPase is much shorter than any known Clp ATPases. Histidine tagged ClpL was overexpressed and purified from E. coli. Immunoblot analysis employing antisera raised against pneumococcus p84 demonstrated no cross-reactivity with Clp analog in Eschericha coli, Staphylococcus aureus and human HeLa cells. Preimmunization of mice with ClpL extended mice life partially but did not protect them from death.
The Effects of Self-administration of Methamphetamine on Serotonin Receptors Level in Rat Brain
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 88~95
(+)-Methamphetamine (METH) is a psychostimulant, which has been the most popular abused drug in Korea. The rewarding mechanism in METH abuse has been reported to be mediated by dopaminergic system. Recently, it has been reported that dopamine releaser (phentermine) plays a dominant role in the discriminative stimulus effects of METH, whereas 5-HT releaser (fenfluramine) can strongly modify METH self-administration. The present study is designed to assess the behavioral changes and the changes of the serotonin receptors in the brains of rats administered repeated of self-administered METH. The repeated administration of 1.0 mg/kg/day METH for 12 days increased locomotor activities, and there was no difference between i.v. and i.p. treatment. Rats had actively acquired METH self-administration for 3 weeks at 0.1 or 0.2 mg/kg/injection. Whereas, it was taken few days to acquire sucrose pellet self-administration. The binding of [
receptors) and [
receptors) to brain sections was examined. Both passive administration and self-administration of METH did not change significantly the serotonin receptors levels in hippocampus, striatum and nucleus accumbens. These results suggest that serotonin receptors may not change in the acquisition period of METH self-administration, and we are trying to investigate the serotonin receptors levels of brain in rats maintained of METH self-administration.n.n.
Influence of SKP 450, a
Channel Opener, on the Pressor Actions Induced by Norepinephrine, Angiotensin II and Carotid Artery Occlusion in Rats
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 96~103
These studies were investigated about influence of SKP 450, a
channel opener, on the pressor actions induced by norepinephrine, angiotensin II and carotid artery occlusion in rats. Before these studies, effect of SKP 450 itself on blood pressure was examinated. SKP 450 produced the depressor action in proportionaly to dose of 0.3, 1.0 and 3.0
g/kg given intravenously and this depressor action was weakened by pretreatment of glibenclamide, a
channel blocker. The pressor action induced by norepinephrine, an alpha-adrenergic agonist, was blocked 1 hr after administation of SKP 450 in a dose of 3.0
/kg, i.v. and directly after in a dose of 6.0
/kg, i.v.. The pressor action induced by angiotensin II was blocked immediatly after treatment of SKP 450 in a dose of 3.0
/kg, i.v.. The pressor action caused by carotid artery occlusion was not affected by SKP 450 of 3.0
/kg, i.v., whereas markedly blocked by SKP 450 of 6.0
/㎦, i.v.. The potentiated-pressor actions of norepinephrine and angiotensin II by pretreatment of chlorisondamine, a autonomic ganglionic blocking agent, were also blocked by administration of SKP 450 in a dose of 6.0
/kg, i.v.. The weakened-pressor action of carotid artery occlusion by pretreatment of chlorisondamine was more weakened by SKP 450 6.0
/kg, i.v.. The results suggest that hyperpolarization formed through
channel opening in cell membrane inhibits the pressor action induced norepinephrine ; angiotensin II ; and carotid artery occlusion.usion.
Studies on the Antihypercholesterolemic Effects of Gamigwaruhaebaekwhanggum - Tang
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 104~111
Gamigwaruhaebaekwhanggum-Tang (GGHWT) have been evaluated for antihyperlipidemic effects on experimental hyperlipidemic rats and mice induced by Triton WR-1339, com oil and high cholersterol-diet. Especially, GGHWT is formulated with Trichosanthis Fructus, Pinelliae Tuber, Aurantii Immaturus Fructus, Magnoliae Cortex, Allii Macrostemi Bulbuls, Cinnamomi Ramulus and Scutellariae Radix. Oral administration of GGHWT at 500 mg/kg/day for 3 days significantly inhibited the increase of serum triglyceride and LDL-cholesterol, liver triglyceride in hyperlipidemic rats induced by Triton WR-1339. And, GGHWT significantly inhibited the increase of serum triglyceride in hyperlipidemic rats induced by corn oil. Also, administration of GGHWT (500 mg/kg, once daily for 1 week, p.o.) prevented the increase of serum total cholesterol, triglyceride, LDL-cholesterol, liver total cholesterol and triglyceride in 1% cholesterol-diet fed mice. These results suggest that GGHWT is effective for the treatment of hyperlipidemia.
Effects of Malloti Cortex Water Extract, Bergenin, and Acetylbergenin on Liver Fibrosis Induced by Bile Duct Ligation in Rats
Chung, Myeon-Woo ; Sunoo, Sub ; Kim, Seung-Hwan ; Kim, Hack-Seang ;
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 112~118
The effects of Malloti Cortex Water Extract (MCWE), bergenin (isolated as an active component from MCWE), and acetylbergenin (synthesized from acetylation of bergenin) on the liver fibrosis induced by bile duct ligation (BDL) in rats. We studied hydroxypro1ine (HYP) as a marker of collagen accumulation in the liver, alanine aminotransferase (s-ALT), aspartate aminotransferase (s-AST), and alkaline phosphatase (s-ALP) as serum markers of liver cell damage induced by BDL, MCWE, bergenin, and acetylbergenin decreased towards normal the accumulated levels of HYP in the liver and the elevated serum levels of s-ALT, s-AST and 5-ALP. The results indicate that MCWE, bergenin, and acetylbergenin ameliorated the liver damage induced by BDL in rats.
Responsiveness of the Thoracic Aorta in Rats Treated with Dehydroepiandrosterone (DHEA)
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 119~124
In order to determine the role of dehydroepiandrosterone (DHEA), the important sex-steroid hormone precursor, in vascular reactivity in rats, animals were treated for two weeks with DHEA or sex hormones, and the vascorelaxant and contractile responses of isolated aorta were examined. DHEA diminished the acetylcholine (ACh)-induced relaxation in female rats, while the drug was without effect in males. Testoterone lowered the vasorelaxant activity to ACh in either sex. 17
-Estradiol enhanced ACh-induced vasorelaxation in male rats, but this female sex hormone did not influence in females. In male rats, the androgen receptor antagonist flutamide also enhanced vasorelaxant action of ACh. When the male rat aorta was incubated in vitro with a nitric oxide (NO) synthase inhibitor L-NAME, phenylephrine-induced contraction was greatly potentiated in DHEA-pretreated rats compared to control ones. The present results suggest that DHEA stimulates mainly androgen in female, but both androgen and estrogen in male rats. The participation of NO In the modulation of vascular reactivity with pretreated DHEA was also considered.
Anxiolytic Effects of the Three Kinds of Traditional Chinese Medicine, Shin-Ki-Hwan, Bo-Jung-lk-Ki-Tang, and Sa-Mul-Tang, Using the Elevated Plus-maze Test
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 125~130
Shin-Ki-Hwan (Shen-Qi-Wan, SKH), Bo-Jung-Ik-Ki-Tang (Bu-Zhong-Yi-Qi-Tang, BJIKT), and Sa-Mul-Tang (Si-Wu-Tang, SMT) have been used for various kinds of deficiency syndromes, such as 'yang', 'qi', and 'blood', respectively. The objects of this study were to determine the effects of water extracts of three different kinds of traditional Chinese medicine (TCM), SKH, BJIKT, and SMT, on the anxiolytic activities in the elevated plus-maze test and to clarify the differences among 'yang', 'qi', and 'blood'. The water extracts of SKH, BJIKT, and SMT were orally administered to male SD rats, at 1.0 g/kg for 10 days. All rats were subjected to behavioral tests for the anxiolytic activity at 10 days. SKH, for the benefiting 'yang'agents, significantly increased the ratio of open arms entry to the total arms entry and time spent in the open arms (p<0.05), suggesting anxiolytic effect. However, both BJIKT and SMT decreased the ratio of open arms entry to the total arms entry and increased times spent in the closed arms (p<0.05). From these findings, it can be speculated that SKH only exhibits anxiolytic effect and that the different anxiolytic effects in the elevated plus-maze test may be come from the meanings of 'yang', 'qi', and 'blood'in oriental diagnostics though the cases are restricted.
The Effect of 52 week Lamivudine Therapy in Patients with Chronic Hepatitis B
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 131~139
Lamivudine, an oral nucleoside analogue, effectively inhibits hepatitis B virus replication and reduces hepatic necroinflammation in patients with chronic hepatitis B. Although lamivudine has shown a promise in patients with chronic hepatitis B, a long-term data on Korean patients with hepatitis B are lacking. The purpose of this study is to evaluate the effects and safety of 52-week lamivudine therapy in Korean patients with chronic hepatitis B, A total of twenty-nine patients (27 male and 2 female) who had received 100 mg of oral lamivudine daily for 52 weeks were evaluated, retrospectively. The mean age of 29 patients in the study group was 37.7
8.9 years (range 19-54). Pretreatment HBV PCR and HBsAg were positive in all 29 patients, and HBeAg were positive in 25 patients (86%). The serum HBV DNA of 28 patients (97%) significantly fell to undetectable levels (<5 pg/ml) within 12 weeks of therapy and it remained undetectable in 24 patients (83%) by the end of 52-week therapy (p<0.001). Mean serum ALT levels of 29 patients declined to the normal range within 12 weeks and remained within the normal range during the evaluative period (p<0.05). The proportions of patients with HBeAg seroconversion (loss of HBeAg, development of antibody to HBeAg, and undetectable HBV DNA) were 42% after 52-week therapy. The differences of response to lamivudine therapy in HBeAg- positive and HBeAg-negative patients were negligible (p>0.05). Furthermore, the study showed that pretreatment serum HBV DNA and ALT levels have no effect to the efficacy of lamivudine therapy (p>0.05). Further comparison of lamivudine's efficacy showed that lamivudine is just as efficacious in patients with cirrhosis as without cirrhosis (p>0.05). In conclusion, lamivudine is an effective and safe therapy for the treatment of chronic hepatitis B in Korean patients.
Single Dose Oral Toxicity Study of A New Hepatotherapeutic Agent GODEX (HEFADIF-S) in Rats
Biomolecules & Therapeutics, volume 9, issue 2, 2001, Pages 140~142
This study was performed to evaluate an single dose oral toxicity of a new hepatotherapeutic agent GODEX (HEPADIF-S) in Sprague-Dawley rats. Male and female rats were administered dosages of 5, 2.5, 1.25 ,0.625, 0.3125, and 0 g/kg B.W. of GODEX, respectively. After single oral administration of GODEX to rats, we observed them daily for 2 weeks. GODEX slid not induce any toxic signs in the mortalities, clinical signs, body weight changes, and gross necropsy findings of rats. Based on these results, it is concluded that GODEX may have no side effect and its LD
value may be over 5 g/kg B.W, in rats.s.