• Title/Summary/Keyword: pharmaceutical activity

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Polyacrylamide Gel Immobilization of Porcine Liver Esterase for the Enantioselective Production of Levofloxacin

  • Lee, Sang-Yoon;Min, Byung-Hyuk;Song, Seong-Won;Oh, Sun-Young;Lim, Sang-Min;Kim, Sang-Lin;Kim, Dong-Il
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.6 no.3
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    • pp.179-182
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    • 2001
  • Porcine liver esterase was immobilized in polyacrylamide gel for the enantioselective production of levofloxacin from ofloxacin butyl ester. The initial activity of immobilized esterase was found to be significantly affected by the polyacrylamide gel composition. The optimum concentrations of monomer and crosslinker were determined to be 20% and 8.3%, respectively. The activity of immobilized esterase was 55.4% compared to a free enzyme. Enantiomeric excess was maintained at 60%, almost the same level as that of free enzyme. In addition, the immobilized esterase could be used repeatedly up to 10 times without experiencing any severe loss of activity and enantioselectivity.

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Assessment of antibacterial activity of the cardiovascular drug nifedipine

  • Pal, Tapas;Dutta, Noton Kumar;Mazumdar, Kaushiki;Dasgupta, Asish;L., Jeyaseeli;Dastidar, Sujata G.
    • Advances in Traditional Medicine
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    • v.6 no.2
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    • pp.126-133
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    • 2006
  • The cardiovascular drug nifedipine exhibited significant in vitro and in vivo antibacterial activity against 331 strains of bacteria belonging to three Gram-positive and twelve Gram-negative genera. The minimum inhibitory concentration of the drug, as determined both by agar and broth dilution methods, was seen to range from $25\;-\;200\;{\mu}g/ml$ against most test bacteria, including several pathogenic ones, in the in vitro studies. Nifedipine was bacteriostatic in action. in vivo studies with this drug showed that it could offer statistically significant protection (P < 0.001) to mice challenged with a virulent bacterium. Therefore, nifedipine has the potential of an antibacterial agent, which may be developed after further pharmacological studies.

Constituents of the Stems of Rumex japonicus with Advanced Glycation End Products (AGEs) and Rat Lens Aldose Reductase (RLAR) Inhibitory Activity

  • Kim, Jong-Min;Lee, Yun-Mi;Jang, Dae-Sik;Kim, Jin-Sook
    • Journal of Applied Biological Chemistry
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    • v.49 no.1
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    • pp.24-27
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    • 2006
  • Four ursane-type triterpenoids, 2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-4(23),12-dien-28-oic acid (1), 4(R),23-epoxy-2${\alpha}$,3${\alpha}$,19${\alpha}$-trihydroxy-24-norurs-12-en-28-oic acid (2), myrianthic acid (3), and tormentic acid (4), and a phenolic compound, ethyl gallate (5), from an EtOAc-soluble extract of the stems of Rumex japonicus, were subjected to in vitro bioassays to evaluate advanced glycation end products (AGEs) and rat lens aldose reductase (RLAR) inhibitory activity. Compounds 1 and 5 exhibited a significant inhibitory activity on AGEs formation with $IC_{50}$ value of 87 ${\mu}M$ and on RLAR with $IC_{50}$ value of 14.3 ${\mu}M$, respectively. Ethyl gallate (5) was isolated for the first time from this plant.

The effect of G009 on lipidperoxidation in rat liver microsome

  • Lee, June-Woo;Jeong, Hoon;Han, Man-Deuk;Kim, Su-Ung;Lee, Seung-Yong;Kim, Kee-Nam;Chung, Sung-Kyun;Baek, Seong-Jin;Song, Jae-Jin;Kim, Yong-Seok;Kang, Sang-Mo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1995.04a
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    • pp.107-107
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    • 1995
  • The purpose of this study was to observe the effects of the polysaccharide(G009) obtained from liquid cultured Ganoderma lucidum IY009 on the lipidperoxidation in rat liver microsome. It is well known that the polysaccharide of G. lucidum have the hepatoprotective activity, antitumor activity etc., which was thought to have the relationship to anti-lipidperoxidation. In order to the estimate the effects of anti-lipidperoxidation of the polysaccharide obtained from G. lucidum IY009, enzymatic and nonenzymatic reaction were performed, in vitro, in rat liver microsome. In enzymatic lipid peroxidation reaction by ADP/FeCl$_3$/NADPH and $CCl_4$/NADPH, G009(1mg/ml) inhibited 77.4%, 39.4%, respectively, and the nonenzymatic reaction strongly exhibited 97.4% inhibition. And also, in enzymatic and nonenzymatic inducers treated with G009, the formation of MDA was progressively greater decreased by raising G009 concentration. These results suggest that anti-lipidperoxidation by G009 treatment may be play an important part in liver protection action.

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Cytotoxic Constituents form the Roots of Anthriscus sylvestris

  • Lim, Young-Hee;Leem, Moon-Jeong;Shin, Dong-Hyuk;Chang, Hwan-Bong;Hong, Seung-Woo;Moon, Eun-Yi;Lee, Dug-Keun;Yoon, Sung-June;Woo, Won-Sick
    • Archives of Pharmacal Research
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    • v.22 no.2
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    • pp.208-212
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    • 1999
  • Activity-guided fractionation of the roots of Anthriscus sylvestris resulted in the isolated and characterization of five cytotoxic compounds, deoxypodophyllotoxin (1), falcarindiol (2), and angeloyl podophyllotoxin (5) from the hexane soluble fraction and morelensin (3), bursehernin (4) from the choloroform soluble fraction. It is the first report of the occurrence of compound 5 in nature.

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The Effects of Scutellaria baicalensis and Scutellaria baicalensis metabolite on Anxiety in the Elevated Plus-Maze in Rats

  • Jung, Ji-Wook;Ahn, Nam-Yoon;Oh, Hye-Rim;Park, Sung-Hwan;Oh, Jin-Kyung;Lee, Bo-Kyung;Kim, Dong-Hyun;Ryu, Jong-Hoon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.211.3-212
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    • 2003
  • Scutellaria baicalensis Georgi is one of the most important medicinal herbs in traditional chinese medicine. The object of this study was to determine the effects of water extracts of Scutellaria baicalensis (SB) and Scutellaria baicalensis metabolite (SBM) on the anxiolytic-like activities in the elevated plus-maze (EPM) test. The water extracts of SB (100, 200, or 400 mg/kg), and SBM (100 mg/kg) were orally administered to male SD rats for 3 day. All rats were subjected to behavioral tests for the anxiolytic activity at 3 days. (omitted)

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Analysis of Studies on Ojeok-san for Establishment of Evidence Based Medicine (EBM 기반 구축을 위한 오적산 연구 논문 분석)

  • Lee, Nam-Hun;Ha, Hye-Kyung;Lee, Ho-Young;Jung, Da-Young;Choi, Ji-Yoon;Lee, Jun-Kyoung;Shin, Hyun-Kyoo
    • Herbal Formula Science
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    • v.16 no.2
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    • pp.1-9
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    • 2008
  • Objective : The purpose of this report was to provide the information about activity and safety of Ojeok-san by analyzing domestic/international papers about Ojeok-san. Methods : Domestic/international papers related to Ojeok-san were reviewed and analyzed. These papers were then classified by year, experimental method and subject. Results : The following results were obtained in this study. 1. The studies of Ojeok-san started from 1984 and has continuously increased. The studies were mainly focused on experimental models rather than clinical studies. 2. By subject, papers related to safety were most common with 5 papers among 20 papers. Besides there were papers related to efficacy of analgesic, anti-hyperlipidemic, anti-blood stasis and treatment for uterine myoma. 3. The papers related to safety were mainly focused on the effect of Okeok-san on liver function, renal function or metal concentration of organs such as blood, brain, liver, kidney and bone. Ojeok-san proved to be safe, but more clinical studies regarding the safety are needed hereafter. 4. Papers related to analgesic, anti-pyretic, anti-phlogistic activities of Ojeok-san were in vivo studies, and other papers were about anti-hyperlipidemic activity, apoptosis inducing activity on uterine myeloma cell line and anti blood static activity on hydrocortisone acetate induced blood statis model. 5. Case reports were about anti-lipidemia, analgesic effect for mastalgia/back pain and anxiety disorder due to climacteric changes. Conclusion : Ojeok-san is being used in various ways with analgesic, anti-pyretic, anti-phlogistic, anti-hyperlipidemic, anti-tumor or anti-blood statis activity. However, mechanism study should be conducted at the molecular biology level and more clinical studies on the efficacy of Ojeok-san are needed.

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Biological activities of ethanol extract from the seawater algae, Chlorella elliposidea C020 (해수클로렐라 [Chlorella elliposidea C020] 에탄올 추출물에 대한 생리 활성)

  • Kim, Hyun-Jin;Kim, In-Hae;Lee, Jae-Hwa
    • KSBB Journal
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    • v.23 no.2
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    • pp.125-130
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    • 2008
  • We investigated the biological activities of ethanol extract from the seawater algae, Chlorella elliposidea C020 such as antibacterial activity, anti-oxidant activity, tyrosinase inhibitory activity and hemolytic activity against human erythrocytes. Extract was obtained from various solvent, methanol, ethanol, acetone and ethanol + acetone (1:1, v/v%), 95% ethanol proved to be best extraction solvents. The contents of ethanol extract were higher in freeze-dried sample than that in frozen-thawing. Antibacterial activities of ethanol extract showed strong inhibitory effect against Bacillus subtilis PM125, Bacillus licheniformis and fish pathogenic bacteria, Vibrio parahaemolyticus KCTC2471 and Edward tarda NUF251. However, this extract didn't worked against antifungal activity against Candida albicans KCTC1940. And, ethanol extract was without hemolytic activity against human erythorocytes. The ethanol extract showed 75% of free radical scavanging effect on 2.0 mg/mL using DPPH method. In tyrosinase inhibition assay of ethanol extract, $IC_{50}$ (Inhibition Concentration) was measured as 10.87 mg/mL. Conclusionally, ethanol extract of Chlorella elliposidea C020 has good candidate for bioactive materials.

Studies on the Mechanism of Action of the Gastric $H^{+}$+$K^{+}$ ATPase Inhibitor KH 3218

  • Cheon, Hyae-Cyeong;Kim, Hyo-Jung;Yum, Eul-Kgun;Cho, Sung-Yun;Kim, Do-Yeob;Yang, Sung-Il
    • Biomolecules & Therapeutics
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    • v.3 no.3
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    • pp.205-209
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    • 1995
  • The novel compound KH 3218 was synthesized and evaluated for its ability to inhibit the gastric H$^{+}$$K^{+}$ ATPase activity in vitro as well as to lessen gastric acid secretion in vivo. KH 3218 inhibited rabbit gastric H$^{+}$$K^{+}$ ATPase in a concentration and time dependent manner. $IC_{50}$/ value was estimated to be about 15 $\mu$M. The inhibition of the H$^{+}$$K^{+}$ ATPase by KH 3218 was blocked by sulfhydryl reducing agents, dithiothreitol or $\beta$-mercaptoethanol. The inhibition of the enzyme was not reversible by 50 fold dilution of the incubation mixtures, suggesting the irreversible nature of the inactivation. In the pylorus-ligated rift, KH 3218 reduced the total acid output as compared with the control. In addition, KH 3218 was capable of inhibiting H. pylori urease activity. These data suggest that KH 3218 is a potent inhibitor for H$^{+}$$K^{+}$ ATPase activity as well as for gastric acid secretion, and has a potential to be developed as a novel antiulcer agent.

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In vitro Evaluation of Anti-Human Immunodeficiency Virus Activity of Nucleoside Derivatives and Studies on Their Mode of Action (핵산유도체들의 항 Human Immunodeficiency Virus in vitro 약효평가와 작용기전연구)

  • Lee, Chong-Kyo;Kim, Dong-Ki;Kim, Jee-Hyun;Kim, Hae-Soo;Pi, Mi-Kyoung;Park, Jong-Beak;Kim, Baek
    • The Journal of Korean Society of Virology
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    • v.27 no.1
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    • pp.69-75
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    • 1997
  • To evaluate in vitro anti-HIV efficacies of nucleoside derivatives, MT-4 cell line was infected with HIV-1 and HIV-2 respectively and treated with various compounds and the formerly approved drugs such as AZT, d4T, ddC and ddI. CPE method was used to evaluate their antiviral activity. Most dideoxynucleosides, AZT, d4T, ddC and ddI, showed anti-HIV activities against both viruses but no other compounds including anti-herpesvirus drugs did any. Further experiments were carried out to study their inhibitory mechanism of viral adsorption. The results showed no inhibition of syncytium formation due to an interaction between the gp120 expressed in HIV -infected cell surface and CD4 receptor on the uninfected cell surface in the presence of AZT. AZT showed no activity up to $100\;{\mu}g/ml$. Inhibition of reverse transcriptase (RT) in the presence of AZT-triphosphate was tested by using RT expressed in E. coli and purified and its $IC_{50}$ was 4.5 nM.

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