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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 effect of gingerol on cytochrome P450 (CYP450) and CYP2E1 and CYP3A activity in mouse liver. Methods: Gingerol (200, 100, 50 mg.kg-1.d-1) was orally administered to mice and liver microsomes were prepared by calcium precipitation after 5 days. The effects of gingerol on hepatic weight, microsomal protein, CYP450 and CYPb5 levels; aminopyrine and erythromycin method for the determination of liver microsomal CYP subtypes CYP2E1 and CYP3A activity. Results: Ginger high, medium and low dose (200,100,50 mg.kg-1.d-1) had no effect on the liver weight and protein content of mice, which could significantly reduce the content of CYP450 and increase the content of CYPb5 (P <0.01 ). The three doses of gingerol both inhibited the activity of CYP2E1 (P <0.05). With the increase of dosage, the inhibition of CYP2E1 was enhanced. High doses of Gingerol could inhibit the activity of CYP3A (P <0.05). CONCLUSION: Gingerol has inhibitory effect on CYP450 content and CYP2E1 and CYP3A activity in mice, and the degree of inhibition is dose-dependent.