2009•Zhongguo linchuang yaolixue yu zhiliaoxueRequires access

Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A

Cheng Guo

Abstract

AIM:To investigate the inhibition of Dengzhanxixin injection on rat liver microsome CYP3A in vitro. METHODS:The rat liver microsomes were incubated with different doses of Dengzhanxixin injection at the present of testosterone,a specific substrate of CYP3A,whose metabolite (6β-hydroxytestosterone) in incubation systems was measuered by HPLC to estimate the effect of Dengzhanxixin injection on the activity of CYP3A in rat liver microsome. Ketoconazole was used as a positive control. RESULTS:In in vitro incubation systems,Dengzhanxixin injection has inhibition on rat liver microsomal CYP3A,the IC50 value and Ki value are 0.40% and 0.24% (V/V),respectively. CONCLUSION:Dengzhanxixin injection which can depress CYP3A activity,is a mixed inhibitor to CYP3A.

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Key concepts: Microsome, CYP3A, Ketoconazole, Incubation, Metabolite, Chemistry, Pharmacology, IC50