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

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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
South Korea
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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