Cocktail法评价注射用益气复脉(冻干)对大鼠肝微粒体CYP1A2、CYP3A的诱导作用

目的:研究注射用益气复脉(冻干)Yi Qi Fu Mai Injection(YQFM)(Lyophilized)对大鼠肝微粒体CYP1A2、CYP3A的诱导作用。方法:将wistar大鼠分为生理盐水对照组,苯巴比妥钠诱导组,YQFM组,连续给药7天后处死,制备肝微粒体。采用Cocktail法,将特异性探针底物非那西丁(CYP1A2)、睾酮(CYP3A)与肝微粒体共孵育,采用高效液相色谱测定孵育所得代谢产物对乙酰氨基酚和6β-羟基睾酮的生成速率,来评价YQFM对CYP1A2、CYP3A的诱导作用。结果:空白对照组、诱导组和YQFM组的对乙酰氨基酚的生成速率分别为(18.04±1.00)、(43.07±2.90)、(27.6±4.5)ng.(mg pro-tein)-1.min-1,6β-羟基睾酮的生成速率分别为(15.79±1.43)、(40.86±3.32)、(32.8±3.67)ng.(mg protein)-1.min-1。结论:YQFM对大鼠肝微粒体CYP1A2、CYP3A有诱导作用。

Effect of Yi Qi Fu Mai(YQFM)(Lyophilized)on the Activity of Hepatic CYP1A2 and CYP3A in Rats

Objective:To investigate the effect of Yi Qi Fu Mai Injection(YQFM)(Lyophilized) on the activity of cytochrome P450(CYP1A2,CYP3A) in rats. Method: Healthy wistar rats raised ethically were pretreated with YOFM(Lophhilized) via the caudal vein once daily for consecutive seven days,and then hepatic microsomes were prepared.A cocktail selective substrates consisting of the phenacetin(PN,CYP1A2) and testosterone(TS,CYP3A) was incubated with rat livermicrosomes.Determined by HPLC method,the formation rates of acetaminophen and 6β-OH testosterone,the metabolites of the probe drugs were used as an indicator to estimate the activity of CYP1A2 and CYP3A.Result: The formation rates of acetaminophen were(18.04±1.00),(43.07±2.90),(27.6±4.5) ng·(mg protein)-1·min-1,The formation rates of 6β-OH testosterone were(15.79±1.43),(40.86±3.32),(32.8±3.67)ng·(mg protein)-1·min-1.Conclusion: YQFM has an induced effect on the activity of CYP1A2 and CYP3A.