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【答案】应助回帖
★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★ ★
感谢参与，应助指数 +1
kltscl: 金币+20, ★★★★★最佳答案 2017-10-09 11:00:17
心静_依然: LS-EPI+1, 感谢应助 2017-10-09 11:57:33
10.1177/1060028017719715 未检索到
ANNALS OF PHARMACOTHERAPY 卷: 51 期: 9 页: 725-734 出版年: SEP 2017
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标题: The Effect of Vinpocetine on Human Cytochrome P450 Isoenzymes by Using a Cocktail Method
作者: Kong, LT (Kong, Lingti); Song, CL (Song, Chunli); Ye, LH (Ye, Linhu); Guo, DH (Guo, Daohua); Yu, ML (Yu, Meiling); Xing, R (Xing, Rong)
来源出版物: EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE 文献号: 5017135 DOI: 10.1155/2016/5017135 出版年: 2016
摘要: Vinpocetine is a derivative of the alkaloid vincamine, which had been prescribed for chronic cerebral vascular ischemia and acute ischemic stroke or used as a dietary supplement for its several different mechanisms of biological activities. However, information on the cytochrome P450 (CYP) enzyme-mediated drug metabolism has not been previously studied. The present study was performed to investigate the effects of vinpocetine on CYPs activity, and cocktail method was used, respectively. To evaluate the effects of vinpocetine on the activity of human CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP2E1, human liver microsomes were utilized to incubate with the mixed CYPs probe substrates and the target components. The results indicate that vinpocetine exhibited weak inhibitory effect on the CYP2C9, where the IC50 value is 68.96 mu M, whereas the IC50 values for CYP3A4, CYP2C19, CYP2D6, and CYP2E1 were all over range of 100 mu M, which showed that vinpocetine had no apparent inhibitory effects on these CYPs. In conclusion, the results indicated that drugs metabolized by CYP2C9 coadministrated with vinpocetine may require attention or dose adjustment.
入藏号: WOS:000371519900001
ISSN: 1741-427X
eISSN: 1741-4288
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