刺五加注射液对大鼠肝CYP3A活性的影响

目的:考察刺五加注射液对大鼠肝细胞色素P4503A活性的影响。方法:制备大鼠空白肝微粒体,加入刺五加注射液孵育,HPLC法测定咪达唑仑浓度,计算咪达唑仑代谢速率评价刺五加注射液体外对大鼠CYP3A酶的影响。大鼠随机分为对照组和实验组,分别尾静脉注射生理盐水和刺五加注射液,连续7 d,制备肝微粒体,进行孵育反应,评价刺五加注射液体内对大鼠CYP3A的影响。结果:刺五加注射液体外对大鼠CYP3A酶具有抑制作用,测得刺五加注射液抑制CYP3A酶的IC50为5.00 mL/100mL。大鼠连续7 d静脉注射刺五加注射液,使探针药物咪达唑仑的代谢减少了21.11%。结论:刺五加注射液对大鼠CYP3A的活性有抑制作用。

Effect of Ciwujia injection on the activity of CYP3A in rats

OBJECTIVE To investigate the effect of Ciwujia injection on the activity of CYP3A in rats.METHODS Liver microsomes of rats were prepared and incubated with Ciwujia injection at the presence of midazolam.Metabolic rate of midazolam was determined by HPLC to determine the effect of Ciwujia injection on the activity of CYP3A.20 rats were divided into control group and experiment group randomly.The control group was given sodium chloride and the experimental group was intravenously given Ciwujia injection for 7 d.The rats were killed after the last treatment by decapitation and livers microsomes protein was prepared,then the CYP3A activities was measured by incubation reactions.RESULTS Ciwujia injection was a potential CYP3A inhibitor in vitro,the IC50 was 5.00 mL/100 mL.CONCLUSION The activities of CYP3A were inhibited obviously by administration of Ciwujia injection,It decreased the metabolism of midazolam by 21.11%.