摘要
目的:比较同分异构体齐墩果酸和熊果酸对人肝微粒体CYP450酶的抑制作用。方法:以人肝微粒体孵育体系为模型,加入齐墩果酸或熊果酸与CYP450探针底物共同孵育;以不同浓度的齐墩果酸对不同浓度的CYP3A4探针底物咪达唑仑的抑制,计算抑制率(Ki)。结果:熊果酸对CYP450酶没有明显的抑制作用;齐墩果酸可轻微抑制CYP1A2的活性,明显抑制CYP3A4酶的活性,Ki为39.2μmol.L-1。结论:齐墩果酸对CYP450酶的抑制作用强于熊果酸。
Objective： To compare the inhibitory effect of oleanolic acid and ursolic acid isomers on cytochrome P450. Methods： Oleanolic acid or ursolic acid was incubated together with CYP probe substrate in human liver microsomes, the inhibition ratio （K0 was calculated by comparing the inhibition for different concentrations of oleanolic acid with the different concentrations of midazolam （substrate of CYP3A4）. Results： Ursolic acid had no significant inhibitory effect on CYP450, while oleanolic acid had little inhibitory effect on CYP1A2, and could significantly inhibit CYP3A4 activity （Ki = 39.2μmol·L-1）. Conclusion： The inhibitory effect of oleanolic acid on CYP450 was stronger than that ofursolic acid.
出处
《中国药物应用与监测》
CAS
2012年第4期201-203,210,共4页
Chinese Journal of Drug Application and Monitoring
