• Title/Summary/Keyword: Inhibitory Activity

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Synthesis and iNOS Inhibitory Activities of Thioflavones

  • Dao Tran Thanh;Tuyen Truong Ngoc;Park Haeil
    • Archives of Pharmacal Research
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    • v.28 no.6
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    • pp.652-656
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    • 2005
  • A number of thioflavones has been synthesized and evaluated for their iNOS inhibitory activities. Thiowogonin (6) was obtained from naturally occurring chrysin in 5 steps. Other thioflavones were prepared from the corresponding flavones in a single step by the reaction with Lawesson's reagent. The biological activities of thioflavones were not enhanced by the functional group conversion from carbonyl to thiocarbonyl. Compounds 11 and 13 showed potent. NO inhibitory activity at high concentration (40 uM), leading to the possible development of novel neuroprotective agents based on wogonin.

Isolation of $\alpha$-Glucosidase Inhibitor Producing Soil Microorganism and Inhibitory Effects of Microbial Metabolites on ${\alpha}$-Glucosidase

  • Lee, Jin-Woo;Park, Sung-Sook;Kang, Byoung-Yong;Kim, Kyoung-Je;Ha, Nam-Joo
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.335.3-336
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    • 2002
  • To find ${\alpha}$-Glucosidase Inhibitors produced by Actinomycetes, 20 soil samples were tested and 53 Actimycetes were isolated. One of 53 Actinomycetes (strain PM718) showed very potent inhibitory activity in vitro. The morphological and physiological characteristics of strain PM 718 were investigated. The spore morphology. spore chain morphology and spore surface were observed by scanning electron microscope. The inhibitory activity of strain PM718 in vivo has been studied in mice made hyperglycemia by Streptozotocin treatment. The strain PM718 showed signficant reduction of blood glucose level(more than 30%) in mice loaded with maltose.

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Effects of Chungyulsodokeum on the Experimental Animals on Analgesic, Anti-inflammatory Activity (淸熱消毒飮이 實驗動物의 鎭痛, 消炎에 미치는 影響)

  • Hwang, Deok-Chan;Lin, Gyu-Sang;Lee, Ki-Nam
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.3 no.1
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    • pp.17-24
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    • 1990
  • In order to investigate the effects of Chungylsodokeum on Analgesic, Anti-inflammatory activity were administered. The results were summarized as follows : 1. The Analgesic effect of acetic acid showed inhibitory effect more than Chungyulsodokeum extract 3mg/kg. 2. The Analgesic effect of Hot Plate showed inhibitory effect more than Chungyulsodokeum 100mg/kg. 3. The Anti-inflammatory effect of Acetic acid showed inhibitory effect at Chungyulsodokeum extract 30, 100mg/kg.

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The inhibitory Effect of Sanggenon C from the Root-bark of Morus alba L. on the Growth and the Cellular Adherence of Streptococcus mutans (상백피의 Sanggenon C에 의한 Streptococcus mutans의 생육 및 균부착 저해효과)

  • Park, Won-Jae;Lee, Hyung-Jae;Yang, Seung-Gak
    • YAKHAK HOEJI
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    • v.34 no.6
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    • pp.434-438
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    • 1990
  • The methanolic extract of the root-bark of Morus alba L.(Mulberry tree) has the potent antibacterial activity against Streptococcus mutans. Its active component was identified to be sanggenon C. The active component had stronger anti-bacterial activity than berberine, having minimum inhibitory concentration(MIC) of $25\;{\mu}g/ml$. Moreover, the inhibitory effect of this component on the cellular adherence of Streptococcus mutans to glass surfaces also was more remarkable than that of berberine in the presence of glucosyltransferase(GTase) and sucrose in vitro. These results indicate that sanggenon C may play an important role in inhibiting plaque formation and caries incidence.

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Radiosensitizing and Topoisomerase I Inhibitory Effects of Aloe vera, Formitella fraxinea, and Ulmus davidiana Extracts

  • Lee, Keyong-Ho;Lee, Jae-Hyun;Cho, Choa-Hyoung;Noh, Moon-Jong;Kim, Young-Bum
    • Natural Product Sciences
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    • v.7 no.2
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    • pp.60-62
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    • 2001
  • Ulmus davidiana, Formitella fraxinea, and Aloe vera extracts were detected to have inhibitory effects against topoisomerase I at treatment of $5{\mu}g$. Ulmus davidiana and Aloe vera extracts were found to show inhibitory effect similar to camptothecin, Formitella fraxinea extract was found to have weak activity. We also found the potential use of those extracts as a radiation sensitizer. Radiosensitizing effect at combination treatment was increased more than 2 times at single treatment of radiation, Ulmus davidiana or Formitella fraxinea extracts. Ulmus davidiana and Formitella fraxinea extracts were found to have significant radiosensitizing effect on test tumor cell line. But, Aloe vera extract was not detected to have activity as a radiosensitizer. Ulmus davidiana and Formitella fraxinea extracts are potent radiosensitizers on tumor cell lines and should be considered for further study of active compounds.

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$\alpha$-Glucosidase Inhibition by Culture Broth of Streptomyces sp. NS15 (Streptomyces sp. NS15 배양액에 의한 $\alpha$-Glucosidase 저해)

  • 백남수;김영만
    • The Korean Journal of Food And Nutrition
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    • v.11 no.6
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    • pp.640-646
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    • 1998
  • For the production of nonprotein $\alpha$-glucosidase inhibitor from the Streptomyces sp. NS15 strain, effects of initial optimum pH, nitrogen sources, carbon sources, cationic metal ions, agitation speed and aeration rate were investigated. Initial optimum pH of medium was 7.0. The most effective nitrogen and carbon sources were soybean meal 2.0%(w/v) and glucose 1.6%(w/v), respectively. The cationic metal ins had no stimulating effect on inhibitory activity of $\alpha$-glucosidase except Fe2+. Agitation speed and aeration rate were effective at 400rpm and 1vvm, respectively. In the jar-fermenter cultivation for 4 days under optimal culture conditions, the culture broth showed the inhibitory acitivity of 3,200units/ml, which is 25 times higher than that of basic medium (CYM) for porcine intestinal $\alpha$-glucosidase. The inhibitory activity of $\alpha$-glucosidase reached about 3,200units/ml after 4 days of cultivation and decreased gradually for a further two days.

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Synthesis and Biological Activities of 8-Arylflavones

  • Dao, Tran-Thanh;Kim, Soo-Bae;Sin, Kwan-Seong;Kim, Sang-Hee;Kim, Hyun-Pyo;Park, Hae-Il
    • Archives of Pharmacal Research
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    • v.27 no.3
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    • pp.278-282
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    • 2004
  • A number of 8-arylflavones have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. 8-Arylflavones were obtained from commercially available chrysin via two different synthetic pathways. Most 8-arylflavones exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Functional group replacement at the 8-position of wogonin from methoxy to aryl group caused loss of inhibitory activity. Our present results imply that the functional group at the 8-position of flavones seems to play very important roles for bioactivity.

Inhibitory Effects of Ginseng Components on Rat Lens Aldose Reductase Activities (인삼성분의 Rat Lens Aldose Reductase 활성에 대한 억제효과)

  • Kim, Hack-Seang;Park, Ung-Yang;Seong, Yeon-Hee
    • Journal of Ginseng Research
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    • v.20 no.1
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    • pp.106-110
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    • 1996
  • The present study was undertaken to elucidate the effects of ginseng components on rat lens aldose reductase activity. Ginseng total saponin (GTS) exhibited inhibitory activities on rat lens aldose reductase in a dose-dependent manner. Among ginsenosides, Rf and Rgl showed potent inhibitory activities on rat lens aldose reductase. Lipid soluble fraction also inhibited rat lens aldose reductase activities. These data suggest that ginseng components inhibit rat lens aldose reductase activity in vitro.

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Screening and Partial Purification of Bacteriocins by Strains of Lactobacillus acidophilus Isolated from Human Origin (인체에서 분리된 Lactobacillus acidophilus가 생산하는 박테리오신의 선별과 정제)

  • Kim, Se-Heon;Kim, Yeong-Gyo;Gilliland, S.E.
    • Journal of Dairy Science and Biotechnology
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    • v.15 no.1
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    • pp.21-26
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    • 1997
  • Lactobacillus acidophilus 223, 606, and NCFM-F among 21 isolated from fecal contents of humans demonstrated inhibitory activity attributed to bacteriocin(s). The bacteriocin(s) were heat stable and nondialyzable proteinous compounds and exhibited narrow inhibitory spectra of activity. Neither hydrogen peroxide nor pH were responsible for inhibitory action. All of the producer strains were resistant to their own bacteriocin(s). The bacteriocin(s) were purified by ammonium sulfate precipitation, gel chromatography and ion exchange chromatography for further characterization. The bacteriocin(s) of human origin exhibited similar characteristics.

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Growth Inhibition on the Strain Isolated from Spoiled Red Bean Paste

  • Hwang, Cheol-Seung;Kim, Yong-Suk;Shin, Dong-Hwa
    • Food Science and Biotechnology
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    • v.14 no.1
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    • pp.46-48
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    • 2005
  • Growth inhibitory effects of ethanol extracts of green tea and pine needles on Bacillus stearothermophilus isolated from spoiled red bean paste were detected at concentrations higher than 750 ppm, and antimicrobial activity of pine needle extract was slightly higher than that of green tea exract. Growth inhibitory effect of pine needle extract in nutrient broth adjusted to pH 6.0, water-activity 0.92, and $45\;^{\circ}$Brix was observed at 500 ppm. These results indicated growth of B. stearothermophilus could be inhibited by adding pine needle and green tea extracts.