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标题：Transformation of Ergosterol Peroxide to Cytotoxic Substances by Rat Intestinal Bacteria
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作者：Joo-Sang Lee ; Chao-Mei Ma ; Dong-Ki Park 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2008
卷号：31
期号：5
页码：949-954
DOI：10.1248/bpb.31.949
出版社：The Pharmaceutical Society of Japan
摘要：Ergosterol peroxide (EPO, 1) is a major antitumor sterol produced by edible or medicinal mushrooms. Following oral administration of 1 to rats or anaerobic in vitro incubation of 1 with rat fecal bacteria, three metabolites were detected and their structures were identified to be 5α,6α-epoxyergosta-8(14),22-diene-3β,7α-diol (M1, 2), 5α,6α-epoxyergosta-8,22-diene-3β,7α-diol (M2, 3), and 5α,6α-epoxy-3β-hydroxyergosta-22-ene-7-one (M3, 4) by spectroscopic analysis. Of these, M2 and M3 showed more potent inhibitory activity than the original compound 1 against proliferation of CACO-2, WiDr, DLD-1 and Colo320 human colorectal adenocarcinoma cells. These findings suggest that bacterial metabolites of EPO play a significant role in its cytotoxic activity against human colorectal cancer cells.
关键词：ergosterol peroxide;rat intestinal bacteria;cytotoxic activity