• Title/Summary/Keyword: Inhibitory Activity

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Screening of Potent Anti-dementia Acetylcholinesterase Inhibitor-containing Edible Mushroom Pholiota adiposa and the Optimal Extraction Conditions for the Acetylcholinesterase Inhibitor

  • Kim, Do-Yeon;Bae, Sang-Min;Han, Sang-Min;Lee, Jong-Soo
    • The Korean Journal of Mycology
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    • v.44 no.4
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    • pp.314-317
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    • 2016
  • To develop a new anti-dementia acetylcholinesterase (AChE) inhibitor from edible mushrooms, AChE inhibitory activities were determined on water and ethanol extracts of various edible mushrooms from oriental medicine markets and agriculture markets. As a result, the 70% ethanol extract from Pholiota adiposa fruiting body had the highest AChE inhibitory activity of 30.6, and its water extract also had an AChE inhibitory activity of 23.8%. Therefore, we finally selected P. adiposa as a potent anti-dementia AChE inhibitor-containing mushroom. The AChE inhibitor of P. adiposa was maximally extracted when its fruiting body was treated with water for 3hr at $70^{\circ}C$ and 70% ethanol for 12 hr at $70^{\circ}C$, respectively.

Isolation of Dineolignans, Saucernetin-7 and -8, with Nitric Oxide Inhibitory Activity and NMR assignment from Saururus chinensis

  • Lee, Kyung-Tae;Jung, Hyun-Ju;Park, Hee-Juhn
    • Korean Journal of Plant Resources
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    • v.19 no.6
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    • pp.655-659
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    • 2006
  • Two dineolignans (1,2) with nitric oxide inhibitory activities were isolated from Saururus chinensis (Saururaceae) using silica gel column chromatography. Although the structures, saucernetin-7 (1) and -8 (2), have been already reported, NMR assignment of the two compounds was completed aided by 2D-NMR spectroscopy including $^1H-^1H$ COSY, $^1H-^{13}C$ COSY, HMBC and NOESY NMR spectra. Compounds 1 and 2 exhibited significant nitride oxide inhibitory activity in LPS-induced RAW 264.7 cells with $IC_{50}$ values of $11.3{\mu}M\;and\;7.1{\mu}M$, respectively.

2,4-Diaryl Benzofuro[3,2-b]pyridine Derivatives: Design, Synthesis, and Evaluation of Topoisomerase Inhibitory Activity and Cytotoxicity

  • Thapa, Pritam;Jahng, Yurngdong;Park, Pil-Hoon;Jee, Jun-Goo;Kwon, Youngjoo;Lee, Eung-Seok
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.3073-3082
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    • 2013
  • Designed and synthesized twenty-four 2,4-diaryl benzofuro[3,2-b]pyridine derivatives were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Various aryl groups such as phenyl, 2- or 3- furyl, 2- or 3-thienyl, and 2-pyridyl were substituted at 2- or 4- position of central pyridine. Compounds 8, 12, 13, and 14, with 2-furyl either at 2- or 4- position of central pyridine showed the significant topoisomerase II inhibitory activity at 100 ${\mu}M$.

Cholinesterase Inhibitory Activity of Two Farnesylacetone Derivatives from the Brown Alga Sargassum sagamianum

  • Ryu, Geon-Seek;Park, Soo-Hee;Kim, Eun-Sook;Choi, Byoung-Wook;Ryu, Shi-Yong;Lee, Bong-Ho
    • Archives of Pharmacal Research
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    • v.26 no.10
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    • pp.796-799
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    • 2003
  • Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.

Preparation of Benzoyloxy Benzophenone Derivatives and Their Inhibitory Effects of ICAM-1 Expression

  • Kwon, Eun-Mi;Kim, Cheol-Gi;Goh, Ah-Ra;Park, Jin-Seu;Jun, Jong-Gab
    • Bulletin of the Korean Chemical Society
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    • v.33 no.6
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    • pp.1939-1944
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    • 2012
  • Benzoyloxy benzophenone derivatives were prepared in 3 steps including DCC coupling, Fries rearrangement and esterification from benzoic acids in 24-89% total yields. Among the prepared 12 benzophenone analogues 1a-1l, the compound 1b having three chloro groups at the para position showed maximum inhibitory effects of ICAM-1 expression but, 1a which have no substituents at all showed no inhibitory activity. This study provides the evidences that benzoyloxy benzophenone derivative, 1b may exert its anti-inflammatory activity by suppressing IFN-${\gamma}$-induced ICAM-1 expression.

Synthesis of Ergosterol and 5,6-Dihydroergosterol Glycosides and Their Inhibitory Activities on Lipopolysaccharide-Induced Nitric Oxide Production

  • Park, HoonGyu;Lee, Tae Hoon;Chang, Fei;Kwon, Hyun Ji;Kim, Jiyoung;Kim, Hakwon
    • Bulletin of the Korean Chemical Society
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    • v.34 no.5
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    • pp.1339-1344
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    • 2013
  • We have synthesized several glycosyl ergosterols and 5,6-dihydroergosterols (DHE) and examined their effects on production of nitric oxide (NO) and iNOS protein expression in LPS-treated RAW264.7 macrophage cells. Our results showed that DHE derivatives inhibited production of NO and iNOS protein expression more strongly than ergosterol derivative. Especially, DHE-Glc exhibited most potent inhibitory activity without cytotoxicity up to the concentration of $100{\mu}M$.

INHIBITORY EFFECT OF ARECA CATECHU L. ON THE GROWTH OF STREPTOCOCCUS MUTANS JC-2 (Streptococcus mutans JC--2의 생육에 미치는 빈랑의 억제효과)

  • Lee, Kwang-Hee;Nam, Yong-Ok
    • Restorative Dentistry and Endodontics
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    • v.20 no.2
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    • pp.839-842
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    • 1995
  • In its study, We investigated the effects of Areca catechu L on the growth and acid production of Streptococcus mutans JC-2 in broth system and the activity of glucosyltransferase. The results were summarized as follow; 1. The growth of Streptococcus mutans JC-2 was suppressed by adding Areca catechu L in broth system. Especially, its inhibitory effect was significant at 2,000ppm of concentration. 2. Areca catechu L decreased the acid production of Streptococcus mutans JC-2. Decrease of pH according to acid production was less in presence of Areca catechu L than in absence. 3. Areca catechu L exerted the inhibitory effect against glucosyltransferase activity form Streptococcus mutans JC-2.

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The Study on Depigmentation of Kamikwibi-Tang (가미귀비탕의 미백효과에 관한 연구)

  • Park, Ho-Soon;Kim,Hye-Jung;Kim, Yoon-Bum
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.17 no.2
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    • pp.48-58
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    • 2004
  • Objective: This study was performed to investigate the depigmentation effects of the extracts of Kamikwibi-Tang. Methods Inhibition of tyrosinase activity, melanin production & cell viability in cultured B16 melanoma cells, UV screen and cytoprotective effects on PC12 cells injured by hydrogen peroxide were measured. Results: The extracts of Kamikwibi-Tang did not have any inhibitory effects on tyrosinase activity and did not show any inhibitory effects on melanin production in melanoma cells and also did not have any inhibitory effects on UV screen. But the extracts showed high cytoprotective effects on PC12 cells injured by hydrogen peroxide. Conclusion : These results suggest that Kamikwibi-Tang indrectly inhibits melanin biosynthesis which is involved in hyperpigmentation and could be used as a whitening agent for the skin.

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Screening of Medicinal Plants containing Lipase Inhibitor and Optimal Extraction Conditions (지질분해효소 저해물질 함유 약용식물의 선발 및 저해물질 추출조건)

  • Lee, Jong-Kug;Kang, Min-Gu;Kim, Young-Hun;Lee, Jong-Soo
    • Korean Journal of Medicinal Crop Science
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    • v.20 no.1
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    • pp.1-7
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    • 2012
  • This study was performed to develop new anti-obesity agents for functional foods from medicinal plants and herbs. Methanol extracts from 560 kinds of medicinal plants and herbs, and their lipase inhibitory activities were investigated. Methanol extract from Desmodium oxyphyllum Dc showed the highest lipase inhibitory activity at 74.2%. This lipase inhibitory activity was maximally extracted when powder of Desmodium oxyphyllum Dc was treated with 80% methanol (1 : 20) for 48 h.

Butyrylcholineesterase(BChE) Inhibitors from a Brown Alga Sargassum sp.

  • Park, Soo-Hee;Ryu, Geon-Seek;Choi, Byoung-Wook;Lee, Bong-Ho
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.375.3-375.3
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    • 2002
  • In continuing search for BChE-inhibitory compounds from Korean marine algae. we found a highly potent inhibitory activity in the methanolic extract of Sargassum species. After partition of the MeOH extract between $CHCl_3$ and 30% MeOH. the former layer was subjected to a series of ODS flash chromatography. silica column chromatography. and preparative TLC to afford three compounds (1-3). Detailed structural elucidation of them is in progress. Compound 1 showed potent BChE-inhibitory activity with $IC_{50}$ values of 11 ng/mL. (omitted)

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