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

Hyun A. Kim, Doo Young Yoon, Sang Myung Lee, Seung Hwa Baek, Gyoon Hee Han, Young Hee Kho, Choong Hwan Lee

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Five 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.

Original languageEnglish
Pages (from-to)269-273
Number of pages5
JournalJournal of microbiology and biotechnology
Volume15
Issue number2
Publication statusPublished - 2005 Apr

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Applied Microbiology and Biotechnology

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