Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A

Abstract

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 esti-mate 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 in-cubation 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.

Key words: Dengzhanxixin injection, rat liver microsome, CYP3A, inhibition, drug-drug interaction

CLC Number:

R965.2

HAN Yong-long, YU Qi, MENG Xiang-le, LI Dan, BIAN Ka, GUO Cheng. Inhibition of Dengzhanxixin injection on rat liver microsomal CYP3A[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2009, 14(8): 891-895.

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