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- Title
- Screening and biotransformation of interleukin-1β converting enzyme production inhibitors from Arctii fructus
- Author(s)
- Hyun A Kim; Do Young Yoon; S M Lee; Seung Hwa Baek; G H Han; Yung Hee Kho; Choong Hwan Lee
- Bibliographic Citation
- Journal of Microbiology and Biotechnology, vol. 15, no. 2, pp. 269-273
- Publication Year
- 2005
- 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.
- Keyword
- arctii fructusD10S cellsinterleukin-1β converting enzyme
- ISSN
- 1017-7825
- Publisher
- Korea Soc-Assoc-Inst
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
- Files in This Item:
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