• Title/Summary/Keyword: Activity-guided isolation

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Isolation and Structure Determination of a Cholesterol Esterase Inhibitor from Ganoderma lucidum

  • Kim, Shin-Duk
    • Journal of Microbiology and Biotechnology
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    • v.20 no.11
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    • pp.1521-1523
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    • 2010
  • Bioassay-guided fractionation of a methanol extract of Ganoderma lucidum gave a pure cholesterol esterase inhibitor. On the basis of spectroscopic analysis and comparison with data from the literature, the structure of this compound was identified as $5{\alpha},8{\alpha}$-epidioxyergosta-6,22-dien-$3{\bet}$-ol (compound I). This compound inhibited cholesterol esterase activity with an $IC_{50}$ value of $42{\mu}M$. Lineweaver-Burk plot analysis revealed that compound I is a noncompetitive inhibitor. The findings of this study suggest that compound I may be the active principle of the hypocholesterolemic effect of Ganoderma lucidum.

Inhibitory Constituents of LPS-induced Nitric Oxide Production from Arctium lappa

  • Park, So-Young;Hong, Seong-Su;Han, Xiang-Hua;Ro, Jai-Seup;Hwang, Bang-Yeon
    • Natural Product Sciences
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    • v.11 no.2
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    • pp.85-88
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    • 2005
  • The methanolic extract from the seeds of Arctium lappa was found to inhibit the LPS-induced nitric oxide (NO) production in murine macrophage RAW264.7 cells. Bioassay-guided fractionation of a methylene chloride soluble fraction led to the isolation of three lignan compounds, arctiin (1), arctigenin (2), and lappaol B (3). Their structures were elucidated by UV, IR, MS, and NMR data, as well as by comparison with those of the literatures. Arctigenin (2) and lappaol B (3) had an iNOS inhibitory activity with $IC_{50}$ values of 12.5 and $25.9\;{\mu}M$, respectively.

Antioxidant Properties of Erigeron annuus Extract and Its Three Phenolic Constituents

  • Lee Hee-Jung;Seo Young-Wan
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.11 no.1
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    • pp.13-18
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    • 2006
  • The antioxidant activity of the extract of Erigeron annuus was assessed by means of two different in vitro tests: bleaching of the stable 1,1-diphenyl-2-picrylhydrazyl radical (DPPH test) and the scavenging of authentic peroxynitrite in company with peroxynitrite generation from 3-morpholinosydnonimine (SIN-1). In both tests, the 85% aq. MeOH and n-BuOH soluble fractions of the crude extract showed a significant scavenging effect on peroxynitrite and DPPH radical in comparison to L-ascorbic acid. And bioassay-guided fractionation of the n-BuOH soluble fraction led to the isolation of three compounds: Apigenin (1), quercetin-3-O-glucoside (2), and caffeic acid (3). The structures of the isolated compounds were elucidated on the basis of their spectroscopic data and their antioxidant activities were measured by determining their capacity to scavenge peroxynitrite and the DPPH radical.

A Suppressive Component on Phagocytosis of Murine Peritoneal Macrophage in Aurantii immaturi pericarpium (청피에 함유된 복강 마크로파지의 탐식작용 억제 성분)

  • Eun, Jae-Soon;Kim, Dae-Keun;So, June-No;Zee, Ok-Pyo
    • YAKHAK HOEJI
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    • v.42 no.6
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    • pp.567-571
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    • 1998
  • The phagocytic activity of murine peritoneal macrophage, was determined by lucigenin chemiluminescence and engulfment of fluorescein-conjugated E. coli particle. The acti vity-guided fractionation upon the methylenechloride fraction of Aurantii immaturi pericarpium led to the isolation of a flavonoid, isosinensetin, as a suppressive component of phagocytosis. Isosinensetin suppressed the lucigenin chemiluminescence and the engulfment of fluorescein-conjugated E. coli particles and enhanced the production of nitric oxide in murine peritoneal macrophage.

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In vitro antitumor activity of flavonoids from Sophora flavescens (고삼(苦蔘)의 항암활성(抗癌活性) 및 활성성분(活性成分)에 관한 연구(硏究))

  • Ryu, Shi-Yong
    • Journal of Haehwa Medicine
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    • v.5 no.2
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    • pp.503-507
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    • 1997
  • The cytotoxicity-guided fractionation of the roots of Sophora flavescens (Leguminosae) extracts led to the isolation of fifteen active principles 1~15, responsible for the cytotoxicity against five kinds of cultured human tumor cell lines, i.e., A549(non small cell lung), SK-OV-3(ovary), SK-MEL-2(skin), XF498(central nerve system) and HCT-15(colon), evaluated by SRB method in vitro. Compounds 2~14 were classified as unusual flavonoid occurred exclusively in this species and the proliferation of each examined tumor cells were significantly inhibited during the continuous exposure to compounds 1~15 for 48 hours, respectively.

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Cytotoxic Polyketides from the Marine Sponge Discodermia calyx

  • Shinde, Pramod B.;Mansoor, Tayyab A.;Luo, Xuan;Hong, Jong-Ki;Lee, Chong-O.;Jung, Jee-H.
    • Bulletin of the Korean Chemical Society
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    • v.28 no.6
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    • pp.990-994
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    • 2007
  • Bioassay-guided fractionation of the MeOH extract from the sponge Discodermia calyx collected off the coast of Jeju Island, South Korea, led to the isolation of a polyketide, icadamide C (1), along with previously reported theopederin K (3). Structure elucidation was performed by a combination of high resolution mass and 2D-NMR (principally COSY, HMBC, HSQC, and NOESY) spectroscopy. Stereochemistry of compound 1 was determined as 2R*, 3R*, 6R*, 10S*, 11S*, 12R*, 13S*, 15R* and 2'S by NMR data and Marfey analysis. Isolated metabolites displayed potent cytotoxic activity against a small panel of five human solid tumor cell lines with ED50 values of less than 0.1 μg/mL.

Cytotoxic Constituents from Solidago virga-aurea var. gigantea MIQ

  • Sung, Jong-Hoon;Lee, Jung-Ock;Son, Jong-Kun;Park, No-Sang;Kim, Mi-Ran;Kim, Jae-Gil;Moon, Dong-Cheul
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.633-637
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    • 1999
  • Activity-guided fractionation of the whole plant of Solidago virga-aurea var. gigantea MIQ. (Compositae) has led to the isolation of three cytotoxic compounds, erythrodial-3-acetate (1), $\alpha$-tocopherol-quinone (2), and trans-phytol (3) from the hexane soluble fraction. It is the first report of those compounds from the genus.

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Chemical Constituents from Buddleja officinalis and Their Inhibitory Effects on Nitric Oxide Production

  • Park, Tae Wook;Lee, Chul;Lee, Jin Woo;Jang, Hari;Jin, Qinghao;Lee, Mi Kyeong;Hwang, Bang Yeon
    • Natural Product Sciences
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    • v.22 no.2
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    • pp.129-133
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    • 2016
  • Bioactivity-guided fractionation of a methanolic extract of Buddleja officinalis led to the isolation of two monoterpenes, crocusatin M (1), crocusatin C (2), a flavonoid, acacetin (3), three lignans, lariciresinol (4), pinoresinol (5), and syringaresinol (6), and two triterpenoidal saponins, mimengoside B (7) and songarosaponin A (8). The structures of isolates were identified based on 1D-, 2D-NMR, and MS data analysis. All isolates were tested for their inhibition on LPS-induced NO production in RAW 264.7 cells. As a result, mimengoside B (7) and songarosaponin A (8) showed a mild inhibitory activity of NO production.

Islation of Aldose Reductase Inhibitors from the Flowers of Chrysanthemum boreale

  • Shin, Kuk-Hyun;Kang, Sam-Sik;Seo, Eun-Ah;Shin, Seung-Won
    • Archives of Pharmacal Research
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    • v.18 no.2
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    • pp.65-68
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    • 1995
  • The methanol extract from the whole parts of the flowers of Chrysanthemum boreals was found to exhibit a significant inhibition of a rat lens aldose reductase (RLAR) activity in vitro. Bioassay guided systematic fractionation of the methanol extract led to the isolation of four flavonoids which were identified as acacetin (1), apigenin (II), luteolin (III) and linarin (IV). Compounds I-III were demonstrated to exhibit a significant inhibition of RLAR. Luteolin (II) was found to be the most potent AR inhibitor with $IC_{50}$ value of $5{\times}10^{-7}M$.

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Aromatase Inhibitors from Isodon excisus var. coreanus

  • Jeong, Hyeh-Jean;Chang, Leng-Chee;Kim, Ho-Kyoung;Kim, Il-Hyuk;A.Douglas Kinghorn;John M.Pezzuto
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.243-245
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    • 2000
  • The diethyl ether extract of isodon excisus var. coreanus exhibited significant inhibitory activity in aromatase assay. Bioactivity-guided fractionation of the extract led to the isolation of three active compounds: inflexin(ent-1${\alpha}$-hydroxy-3${\beta}$,6a-diacetoxykau r-16-en-11,15-dione) (1), ursolic acid (2), and ursolic acid 3-O-acetate (3).

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