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目的:研究常用中药单体及其制剂对CYP3A活性的抑制作用。方法:在体外肝微粒体孵育体系中加入底物睾酮和不同浓度的中药单体或其制剂,以高效液相色谱法检测6β羟基睾酮的生成量,计算CYP3A酶活性。用GraphPad Prism v 5.0软件,按照非线性回归计算出药物对CYP3A抑制作用的IC50值。结果:不同中药单体及其制剂对CYP3A抑制作用的IC50值如下:大黄酸IC50值为36.74μmol·L-1;大黄素IC50值为23.09μmol·L-1、芦荟大黄素IC50值为23.91μmol·L-1,蜂胶IC50值为60.3μg·ml-1;水飞蓟素胶囊IC50值为24.5μg·ml-1;丹参酮ⅡA磺酸钠注射液IC50值为0.14%(v/v);五味子酯甲IC50值为0.56μmol·l-1。结论:大黄中的蒽醌、五味子酯甲、蜂胶、水飞蓟胶囊以及丹参酮ⅡA磺酸钠注射液在体外对鼠或人肝CYP3A酶具有抑制作用,临床上使用相关制剂时应密切关注其可能引起的药物相互作用。
Objective: To study the inhibition of CYP3A activity by commonly used traditional Chinese medicine monomers and their preparations. Methods: Substrate testosterone and different concentrations of Chinese traditional medicine monomer or its preparation were added to in vitro liver microsomal incubation system. The production of 6β hydroxytestosterone was detected by HPLC, and the activity of CYP3A was calculated. The IC50 value of the drug on the inhibition of CYP3A was calculated by nonlinear regression using GraphPad Prism v5.0 software. Results: The IC50 values of CYP3A by different traditional Chinese medicine monomers and their preparations were as follows: the IC50 value of rhein was 36.74μmol·L-1; the IC50 value of emodin was 23.09μmol·L-1; the IC50 value of aloe-emodin was 23.91μmol IC 50 of silymarin capsule was 50μg · ml-1; the IC50 value of silybin was 24.5μg · ml-1; the IC50 value of sodium tanshinone ⅡA sodium sulfonate was 0.14% (v / v) Value of 0.56μmol·l-1. Conclusion: Anthraquinone, Schisandra ester, propolis, silymarin capsule and tanshinone Ⅱ A sodium sulfonate injection in rhubarb can inhibit the CYP3A enzyme activity of mouse or human liver in vitro. When using the related preparations clinically, it should pay close attention to its possible Caused by drug interactions.