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学科主题物理化学
Quantitative Determination of the AntiMDR Activities of Ginsenosides
Yang L(杨凌); Wang YL(王玉林); WilfredD.Stein
会议名称The 1st asia Pacific ISSX Meeting
会议日期2006-5-24
2006-05-24
会议地点韩国
页码270/1
部门归属十八室
英文摘要Objective: To understand the MDR reversal activity of the ginsenosides, with quantitative and comparative points of view. Methods: We have utilized K562/ADR and K562/S cell lines in studying the multidrug resistance reversal function of 16 kinds of ginsenosides quantitatively, determining Ki for each one. Results: The sequence of ginsenosides with decreased multidrug resistance reversal activity is Quasipanaxatriol (Qpt), Rc, R-Rg3, Quasipanaxadiol (Qpd), Rg1, Protopanaxatriol (Ppt), Protopanaxadiol (Ppd), Rg2, Re, Rh1 and Compound K (CK). The Ki of Protopanaxatriol, Rc, R-Rg3, Quasipanaxadiol, Rg1 and Protopanaxatriol are at the magnitude of BM, which indicates that they are potential MDR modulators for chemotherapy in the clinic. The MDR reversal activity of Quasipanaxatriol is higher than that of Quasipanaxadiol, and the activity of Protopanaxatriol is higher than that of Protopanaxadiol. The only difference between the two molecules in each pair is in the hydroxyl at C6, which suggests that the substitution of hydroxyl at C-6 could enhance the MDR reversal activity of ginsenosides. Conclusion: Equation IC50=IC0- (IC0-ICs)*C/(Ki+C) is suitable for the primary quantitative determination of MDR modulators in a high throughput screen in drug development. (Supported by the Leading Program of the Chinese Academy of Sciences KGCXZ-SW-213-04)
语种中文
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/112188
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Yang L,Wang YL,WilfredD.Stein. Quantitative Determination of the AntiMDR Activities of Ginsenosides[C],2006:270/1.
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