• 약학회지
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• 제53권4호
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• pp.201-205
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• 2009

In an ongoing investigation into anti-inflammatory compounds from natural products, the $CH_2Cl_2$ soluble fraction of Patrinia scabiosaefolia F. (Valerianaceae) was found to inhibit IL-6 production in TNF-$\alpha$ stimulated MG-63 cell line. By means of a bioassay-directed chromatographic separation technique, lappaol E (1), and nortrachelogenin (2) were isolated. These compounds have been isolated from this plant for the first time. Compounds $1{\sim}2$ showed potent antioxidative activity using NBT superoxide scavenging assay. Moreover, compound 1 decreased IL-6 production in TNF-$\alpha$ stimulated MG-63 cell line.

• Journal of Microbiology and Biotechnology
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• 제15권2호
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• pp.269-273
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• 2005

Five dibenzylbutyrolactones were isolated from a methanol extract of Arctii fructus (Arctium lappa L.) by bioassay-guided isolation, using the interleukin-l $\beta$ converting enzyme (caspase-l, 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-$\beta$-induced proliferation of D 1 OS 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 (IC$_{50}$=74.2$\mu$g/ml), a major component of Arctii fructus, was transformed to aglycone, arctigenin (IC$_{50}$=12.5$\mu$g/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.