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| 常用中药单体及其制剂对CYP3A活性的体外抑制作用研究 |
| Inhibitory Effects of Common Monomers and Related Preparations of Traditional Chinese Medicines on CYP3A Activities in vitro |
| 投稿时间：2014-03-12 修订日期：2014-04-30 |
| DOI： |
| 中文关键词: 中药单体及其制剂 肝微粒体 CYP3A 抑制作用 |
| 英文关键词:Monomers and related preparations of traditional Chinese medicines Liver microsomes CYP3A Inhibition |
| 基金项目:武汉大学自主科研课题（编号：2042014kf0131）;上海市卫生局(编号:2012L058A) |
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| 中文摘要: |
| 摘 要 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 v5.0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36.74 μmol·L-1；大黄素IC50值为23.09 μmol·L-1、芦荟大黄素IC50值为23.91 μmol·L-1，蜂胶IC50值为60.3 μg·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0.56 μmol·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。 |
| 英文摘要: |
| ABSTRACT Objective: To evaluate the effects of common monomers and related preparations of traditional Chinese medicines on the enzyme activity of liver CYP3A. Methods:The monomers and related preparations of traditional Chinese medicines at various concentrations were incubated with liver microsomes and testosterone. CYP3A activity was determined by measuring the amount of 6β-hydroxytestosterone by HPLC. GraphPad Prism v5.0 software was used to calculate the IC50value by nonlinear regression.Results:The IC50 value of CYP3A was 36.74 μmol·L-1 for rhein,23.09 μmol·L-1 for emodin, 23.91 μmol·L-1 for aloe emodin,60.3μg·mL-1for propli,24.5 μg·mL-1 for milk thistle, 0.14%(v/v) for tanshinone ⅡA sulfonate injections and 0.56μmol·L-1 for schisantherin A, respectively. Conclusion:Anthraquinone in rhubarb, schisantherin A, propli, milk thistle and tanshinone ⅡA sulfonate injections can inhibit the enzyme activity of rat or human liver CYP3A in vitro. The related drug interaction should be paid close attention in the clinic use. |
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