大鼠肝微粒体法评价20种中药有效成分对CYP2C9酶的作用.docVIP

大鼠肝微粒体法评价20种中药有效成分对CYP2C9酶的作用 张远冬1，刘学庆1，郭延垒2，张有金2，石亮2，王二豪2，于超（400016重庆重庆医科大学公共卫生学院生殖生物学研究室1生命科学研究院2） 摘要目的方法37 ℃水浴温孵冰乙腈终止反应，HPLC产物4＇-羟基双氯酸结果4＇-羟基双氯酸mol/(min·mg)，显著低于对照组[（735.8±17.27）pmol/(min·mg)，P＜0.05]，其他中药成分实验组与对照组比较，其转化率无统计学差异。结论CYP2C9酶关键词CYP2C9；中药有效成分 [中图法分类号] [文献标志码] A [基金项目国家自然科技重大专项（2010ZX09401-306-1-1）重庆科技创新能力建设项目（CSTC2010AA5058） 通作者于超，E-mail:yuchaom@163.comEffects of CYP2C9 activities in rat live microsomes by 20 active constituents of chinese herbal drugs Zhang Yuandong1，L Xueqing1，G Yanlei2，Z Youjing2，Siang2，W Erhao2，Y Chao (1Reproductive Biology Laboratory，School of Public Health2Institute of Life Sciences，Chongqing Medical University，400016,China) [Abstract] Objective To establish a method for evaluating the activity of cytochrome P450 2C9 using diclofenac as the probe compound in rats liver microsomes (RLM) in vitro, and investigate the impact of 20 active constituents of chinese herbal drugs on CYP2C9 activity. Methods Diclofenac and 20 active constituents of chinese herbal drugs were incubated with rat liver microsomes for 15 min at 37 ℃, and the reaction was terminated by cold acetonitrile, and the theconvert ratio of 4＇-Hydroxydiclofenac determined by HPLC. Finally, the effects of 20 active constituents of chinese herbal drugs on CYP2C9 activities was evaluated by compaired theconvert ratio with control group. Results Among the 20 active constituents, Baicalein, Cnidiadin, Emodin, Swertiamarin, Icariin, Resveratrol were found to have a strong inhibition on CYP2C9 with theconvert ratio of 402.6±10.58, 210.9±10.26, 414.5±10.32, 509.8±26.45, 355.4±15.87, 387.3±22.16[pmol/(min?mg)], which were significantly lower than control group735.8±17.27[pmol/(min?mg), P＜0.05Conclusion The method of rats liver microsomes for evaluating influence of active constituents of chinese herbal drugs on CYP2C9 activity was successfully established. Baicalein, Cnidiadin, Emodin, Swertiamarin, Icariin, Resveratrol have inhibited CYP2C9 activi