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学科主题: 物理化学
题名: Quantitative Determination of the AntiMDR Activities of Ginsenosides
作者: 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
出版日期: 2006-05-24
会议地点: 韩国
通讯作者: 杨凌
部门归属: 十八室
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
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/112188
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Yang L,Wang YL,WilfredD.Stein. Quantitative Determination of the AntiMDR Activities of Ginsenosides[C]. 见:The 1st asia Pacific ISSX Meeting. 韩国. 2006-5-24.
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