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目的:研究绿豆衣提取物(MBSC)对大鼠肝微粒体中细胞色素P450(CYP)3A4酶活性的影响.方法:采用高效液相色谱法,以咪达唑仑为CYP3A4探针药物,建立检测咪达唑仑代谢产物1-羟基咪达唑仑在大鼠肝微粒体孵育体系中浓度的方法,对体外肝微粒体孵育体系中孵育时间、肝微粒体量、孵育时间进行优化,以优化后的条件先后评价绿豆衣提取物对CYP3A4活性的影响及其潜在作用机制.结果:MBSC初提物可显著抑制CYP3A4酶活性,其活性仅为对照组的38.14%(P<0.05),且IC50值为489.7μg·ml-1,抑制机制为竞争-非竞争性抑制.结论:绿豆衣提取物在体外对大鼠CYP3A4酶的活性具有抑制作用,尚需进一步应用体内模型评价其对CYP3A4活性的影响.“,”Objective:To investigate the effect of extract of mung bean seed coat ( MBSC) on the activity of CYP3A4 in vitro. Methods:Midazolam was used as the probe drug, and an HPLC method for determining the metabolite of midazolam ( l-hydroxyl mid-azolam) in rat liver microsome incubation system was established. Three important parameters including the incubation time, concen-tration of rat microsome and probe concentration were optimized for rat liver microsome incubation system, and then the optimal incuba-tion system was applied to study the effect of MBSC extract on CYP3A4 activity and the potential mechanism. Results: The results showed MBSC crude extract could inhibit CYP3A4 activity to 38. 14% as that in the control group(P<0. 05) with IC50 value of 489. 7μg·ml-1 . The mechanism might be related to competition-noncompetition inhibition. Conclusion: MBSC extract exhibits inhibitive potency to CYP3A4 in in-vitro model. Further studies should be conducted to check the influence of MBSC on CYP3A4 in vivo.