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标题：Pharmacokinetics of Ginsenoside Deglycosylated by Intestinal Bacteria and Its Transformation to Biologically Active Fatty Acid Esters
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作者：Hideo HASEGAWA ; Ki-Seung LEE ; Takema NAGAOKA 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：2000
卷号：23
期号：3
页码：298-304
DOI：10.1248/bpb.23.298
出版社：The Pharmaceutical Society of Japan
摘要：Ginsenosides are deglycosylated by intestinal bacteria to active forms after oral administration. The present study demonstrated the pharmacobynamics of 20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol (M1), an intestinal bacterial metabokite of ginsenosides, and the in vitro and in vivo antitumor activities of M1-metabolites in comparison with M1 using C57BL/6 mice and Wistar rats. M1 wsa selectively accumulated into the liver soon after its intravenous administration to mice, and mostly excreted as bile; however, some M1 was transformed to fatty acid ester (EM1) in the liver. EM1 was isolated from rats in a recovery dose of approximately 24 mol%. Structural analysis indicated that EM1 comprised a family of fatty acid mono-esters of M1. Because EM1 was not excreted as bile as M1 was, it was accumulated in the liver longer than M1. Although the cytotoxicity of M1 against B16-F10 melanoma cells was attenuated by fatty acid esterification, EM1 inhibited tumor growth more than M1 in vivo. These results suggest that the fatty acid M1 esters may be the real active principles of ginsenosides in the body.
关键词：ginsenoside;intestinal bacterial metabolite;esterification;biologically acitive fatty acid triterpene ester;active principle