血塞通注射液等36种中药对大鼠CYP2D1的作用

The inhibition of 36 traditional Chinese medicine on rat CYP2D1 activity

目的:研究血塞通注射液等36种中药对大鼠肝微粒体CYP2D1的作用。方法:建立右美沙芬的高效液相-紫外测定方法;以右美沙芬为探针药物,通过考察其体外转化率的变化评价受试中药对大鼠CYP2D1的作用。结果:血塞通注射液、清开灵注射液、银黄口服液、蓝芩口服液使探针药物的转化率分别为(218.7±11.6)pmol/min.mg、(214.9±19.7)pmol/min.mg、(204.3±13.3)pmol/min.mg、(127.0±41.4)pmol/min.mg,显著低于对照组(431.5±4.2)pmol/min.mg,四种药物的IC50分别为1.0ml/100ml、0.6ml/100ml、0.2ml/100ml、0.1ml/100ml。结论:血塞通注射液、清开灵注射液、银黄口服液、蓝芩口服液体外对大鼠CYP2D1有显著抑制作用,且呈浓度依赖性。

Objective： To evaluate the effect of in vitro treatment with 36 kinds of traditional Chinese medicine on activity of CYP2D1 in the liver of male rats.Methods：Using HPLC-UV to determine the activity of CYP2D1 in rat liver microsomes by detecting conversion rate of its substrate-dextromethorphan hydrobromide after treatment with the traditional Chinese medicine in vitro.Results： Xuesaitong Injection（血塞通注射液）,Qingkailing Injection（清开灵注射液）,Yinhuang Oral Liquid（银黄口服液）,Lanqin Oral Liquid（蓝芩口服液） made the conversion rate of dextromethorphan hydrobromide as（218.7±11.6）pmol/min·mg,（214.9±19.6）pmol/min·mg,（204.3±13.3）pmol/min·mg,（127.0±41.4）pmol/min·mg,respectively,which was significantly lower than control group（431.5±4.2）pmol/min·mg（P〈0.05）.And the IC50 values were 1.0ml/100ml,0.6ml/100ml,0.2ml/100ml,0.1ml/100ml,respectively.Conclusion： Xuesaitong Injection,Qingkailing Injection,Yinhuang Oral Liquid,Lanqin Oral Liquid can inhibit the activity of CYP2D1 in a dose-dependent manner in rat liver microsomes in vitro.