상세 정보

underline
Metadata Downloads : dc(xml) or Excel
Cited 0 time in scopus ci

Title 

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

Authors 

Hyun A KimDo Young YoonS M LeeSeung Hwa BaekG H HanYung Hee KhoChoong Hwan Lee

Publisher 

The Korean Society for Applied Microbiology

Issue Date 

2005

Citation 

Journal of Microbiology and Biotechnology, vol. 15, no. 2, pp. 269-273

Keywords 

arctii fructusD10S cellsinterleukin-1β converting enzymearctii lappa extractarctiininterleukin 1beta converting enzymeinterleukin 1beta converting enzyme inhibitorbiotransformationdrug screening

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.

ISSN 

1017-7825

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


There are no files associated with this item.
qrcode

FusionCharts.
DSpace Software Coptright(c) 2010 MIT and Hewleft-Packard  /  KRIBB-REPOSITORY ( Email:jakim@kribb.re.kr)