姜酚对小鼠肝药酶活性的影响

Effect of Gingerol on Mice's Liver Drug Metabolizing Enzyme

目的:研究姜酚对小鼠肝脏细胞色素氧化酶P450(CYP450)含量及其亚型CYP2E1与CYP3A活性的影响。方法:小鼠口服给药姜酚(200,100,50 mg.kg-1.d-1),5 d后钙沉淀法制备肝微粒体,测定并考察姜酚对小鼠肝重、微粒体蛋白、CYP450及CYPb5含量的影响;氨基比林法和红霉素法测定肝微粒体CYP亚型CYP2E1与CYP3A的活性。结果:姜酚高、中、低剂量(200,100,50 mg.kg-1.d-1)对小鼠肝重、蛋白含量无影响,能显著降低CYP450的含量以及增加CYPb5的含量(P<0.01);3种剂量姜酚均可抑制CYP2E1的活性(P<0.05),且随着剂量增加抑制作用增强,高剂量姜酚可以抑制CYP3A的活性(P<0.05)。结论:姜酚对小鼠CYP450含量及亚型CYP2E1,CYP3A活性有抑制作用,抑制程度与剂量有关。

Objective： To study the effects of gingerol on the contents of liver microsomal cytochrome P450 and the activities of CYP2E2 and CYP3A in mice. Method： Gingerol （200, 100, 50 mg-kg-X＇d-1） were ig given to male mice for 5 days, after the liver microsomes were prepared by Calcium isolation, the effects of gingerol on the contents of mice liver heavy, microsomal protein, CYP450 and CYPb5 were determined and the activities of CYP2E2 and CYP3A were tested by using erythromycin and aminopyrine. Result： The gingerol had no effects on the contents of liver heavy and microsomal protein in mice treated with gingerol （200, 100, 50 mg kg-1 d-1） but could markedly decrease and increase the contents of cYPg50 and CYPb5, respectively （P 〈 0.01）; the activity of CYP2E1 was inhibited in mice treated with gingerol （200, 100, 50 mg kg-1 d-1） （p 〈0.05 ） and the effect of inhibition became stronger with the dose increasing of gingerol. The activity of CYP3 A was inhibited in mice treated with gingerol （200 mg kg-l.d-1）, （p 〈0.05）. Conclusion： Gingerol has the effects of inhibiting the content of CYP450 and the activities of CYP2E1 and CYP3A, the degree of inhibition is related to dose.