盐酸小檗碱对大鼠肝微粒体细胞色素P450酶含量及活性的影响

摘要

目的：考察盐酸小檗碱对大鼠肝微粒体的蛋白含量、CYP450酶总量和主要 CYP450酶亚型(CYP1A2、CYP2D6、CYP3A4和 CYP2C19)活性的影响。方法以溶剂为空白对照灌胃给予盐酸小檗碱250 mg/(kg·d),连续7 d,测定其肝微粒体蛋白含量、CYP450蛋白含量以及 CYP1A2、CYP2D6、CYP3A4和CYP2C19活性。结果与空白对照组比较,盐酸小檗碱给药组大鼠肝微粒体蛋白含量及肝微粒体CYP450含量无明显差异(P>0．05)。盐酸小檗碱给药后,给药组大鼠的平均CYP3A4活性是空白对照组的1/2；而两组之间CYP1A2、CYP2D6和 CYP2C19的活性相当。结论盐酸小檗碱对大鼠 CYP3A4活性有一定抑制作用,对CYP1A2、CYP2D6和CYP2C19的活性没有影响。%Objective To study the effect of berberine on the content of livermicrosome protein,cytochrome P450(CYP450)and the activity of CYP1A2,CYP2D6,CYP3A4 and CYP2C19 in cytomicrosome of rat liver. Methods Rats were given berberine by oral administration [250 mg/(kg·d)] for 7 days,and the content of livermicrosome protein,CYP450 and the activity of CYP1A2,CYP2D6,CYP3A4 and CYP2C19 in cytomicrosome were determined taking drug solvent as control group. Results There was no significant difference in the content of livermicrosome pro-tein and CYP450 between control group and treated group. The activity of CYP3A4 in treated group was about half of that of control group, while the activities of CYP2D6, CYP1A2 and CYP2C19 in both groups were compara-ble. Conclusion Berberine has inhibition effect on the activity of CYP3A4,while it shows no effect on CYP2D6, CYP1A2 and CYP2C19 in rats.