罗格列酮对大鼠肝细胞色素P-4502E1活性的影响

目的 :探讨罗格列酮对细胞色素P 4 5 02E1活性的影响。方法 :在正常大鼠肝细胞微粒体中加入浓度为 0 ,0 .10 ,0 .2 5 ,0 .5 0 ,1.0 0mmol·L- 1罗格列酮 ,以N 二甲基亚硝胺为底物 ,测定细胞色素P 4 5 0 2E1活性。另外用 0 ,0 .2 ,2 ,2 0mg·kg- 1剂量的罗格列酮分别对用乙醇诱导和未用乙醇诱导的大鼠灌胃 ,然后取大鼠肝细胞微粒体 ,以N 二甲基亚硝胺为底物 ,测定细胞色素P 4 5 0 2E1活性。结果 :在体外试验中 ,加入不同浓度罗格列酮的大鼠肝微粒体中细胞色素P 4 5 0 2E1活性差异无显著意义。在体内试验中 ,给予不同剂量罗格列酮的大鼠的肝细胞色素P 4 5 0 2E1活性差异也无显著意义 ;结论 :罗格列酮对大鼠的肝细胞色素P 4 5 0 2E1活性无明显影响

Effect of rosiglitazone on activity of cytochrome P-450 2E1 in rat liver

AIM: To investigate the effects of rosiglitazone on the activity of cytochrome P 450 2E1. METHODS: Rosiglitazone in the concentrations of 0,0.10,0.25,0.50,1.00 mmol·L -1 was added into normal rat liver microsomers, and the activities of CYP 450 2E1 in the microsomes were examined with the substrate of N dimethylnitrosoamine. In addition, rosiglitazone in the doses of 0,0.2,2,20 mg·kg -1 was given to rats that had undergone or had not undergone the pretreatment of ethanol induction. Then the rat liver microsomes were isolated, and the activities of CYP 450 2E1 were estimated with the substrate of N dimethylnitrosoamine. RESULTS: In vitro , the activities of CYP 450 2E1 in rat liver microsomes added different concentrations of rosiglitazone had no significant differences. In vivo , the activities of hepatic CYP 450 2E1 of rats that were treated with different doses of rosiglitazone had no significant differences as well. CONCLUSION: Rosiglitazone does not affect the activity of CYP 450 2E1 in rat liver apparently.