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标题：Inhibitory Effects of Ginsenosides and Their Hydrolyzed Metabolites on Daunorubicin Transport in KB-C2 Cells
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作者：Shuji Kitagawa ; Tomoharu Takahashi ; Tomohiro Nabekura 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：2007
卷号：30
期号：10
页码：1979-1981
DOI：10.1248/bpb.30.1979
出版社：The Pharmaceutical Society of Japan
摘要：We studied the effects of ginsenosides and their metabolites on daunorubicin transport in multidrug-resistant P-glycoprotein (P-gp)-overexpressing KB-C2 cells. Ginsenoside Rg1, which is a protopanaxatriol-type ginseng saponin, did not have any effects on the accumulation of P-gp substrate daunorubicin. On the other hand, its metabolite M4, which has no sugar moiety, increased the accumulation 3.6-fold at 5 μ M . Metabolites of protoanaxadiol-type saponin M1 and M12 also increased accumulation, but the effects were less than that of M4. The findings showed larger effects of metabolites without glucose moieties. Analysis of verapamil-stimulated ATPase activity in membrane vesicles expressing human P-gp suggested that the increased daunorubicin accumulation by M4 was at least partly due to ATPase inhibition of P-gp.
关键词：ginsenoside;P-glycoprotein;ATPase;saponin