Screening and biotransformation of interleukin-1β converting enzyme production inhibitors from Arctii fructus

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dc.contributor.authorHyun A Kim-
dc.contributor.authorDo Young Yoon-
dc.contributor.authorS M Lee-
dc.contributor.authorSeung Hwa Baek-
dc.contributor.authorG H Han-
dc.contributor.authorYung Hee Kho-
dc.contributor.authorChoong Hwan Lee-
dc.description.abstractFive dibenzylbutyrolactones were isolated from a methanol extract of Arctii fructus (Arctium lappa L.) by bioassay-guided isolation, using the interleukin-1β converting enzyme (caspase-1, ICE) production inhibitory assay in vitro. These compounds were spectroscopically identified as lappaol E (1), lappaol A (2), matairesinol (3), arctigenin (4), and arctiin (5). Among the compounds tested, arctigenin (4) showed the strongest inhibitory activity for ICE production in IL-1β-induced proliferation of D10S cells. Western blot analysis demonstrated that the arctigenin suppressed the expression of ICE protein in a dose-dependent manner. To estimate the biotransformation of Arctii fructus in vivo by human intestinal bacteria, we carried out an anaerobic incubation of the Arctii fructus extract with a human fecal suspension. From the HPLC analysis of metabolites, Arctiin (IC50=74.2 μg/ml), a major component of Arctii fructus, was transformed to aglycone, arctigenin (IC50=12.5 μg/ml), by human intestinal bacteria. The ICE production inhibitory activity of Arctii fructus would be much stronger in vivo than in vitro due to the biotransformation by human intestinal bacteria.-
dc.publisherSouth Korea-
dc.titleScreening and biotransformation of interleukin-1β converting enzyme production inhibitors from Arctii fructus-
dc.title.alternativeScreening and biotransformation of interleukin-1beta converting enzyme production inhibitors from Arctii fructus-
dc.citation.titleJournal of Microbiology and Biotechnology-
dc.identifier.bibliographicCitationJournal of Microbiology and Biotechnology, vol. 15, no. 2, pp. 269-273-
dc.subject.keywordarctii fructus-
dc.subject.keywordD10S cells-
dc.subject.keywordinterleukin-1β converting enzyme-
dc.subject.localarctii fructus-
dc.subject.localD10S cells-
dc.subject.localinterleukin-1β converting enzyme-
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