乙烷硒啉对H-22荷瘤鼠CYP450酶系影响  

Effect of ethaselen on the content and activity of liver CYP450 enzyme in H-22 tumor bearing mice

作　　者：尹进[1] 尹晗[1] 任晓远[1] 徐静[1] 曾慧慧[1] 

机构地区：[1]北京大学天然药物及仿生药物国家重点实验室,北京100191

出　　处：《中国新药杂志》2009年第18期1783-1786,1797,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(BIA010092-A02);国家自然科学基金(30472036);北京市自然科学基金(7021001)

摘　　要：目的:观察新药乙烷硒啉(BBSKE)对肿瘤H-22引起的小鼠肝脏细胞色素P450含量及其主要亚型活性变化的影响。方法:H-22荷瘤小鼠,给予不同剂量的BBSKE10d后,提取肝微粒体,Omura法测定CYP450的含量,分光光度法测定CYP1A,CYP3A和CYP2E1活性。结果:肿瘤H-22能引起CYP1A活性升高(P<0.01),CYP3A活性降低(P<0.01);BBSKE能明显下调荷瘤鼠CYP1A活性,上调CYP3A活性作用(P<0.05)。肿瘤H-22和BBSKE对CYP450含量和CYP2E1均无明显影响。结论:BBSKE对荷瘤鼠CYP1A活性有下调作用;对CYP3A有诱导作用;对CYP2E1无明显影响。Objective：To assess the effects of ethaselen on rat cytochrome P450 and its main subtypes induced by tumor H-22. Methods：H-22 tumor bearing mice were administered with different doses of BBSKE for 10 days. After the separation of liver microsome, Omura method was used to measure the content of CYP450 while spectrophotometer were selected to detect the activity of CYP1 A, CYP3 and CYP2E1. Results： H-22 tumor significantly increased the activity of CYP1A and decreased that of CYP3A （P 〈 0. Of ）. BBSKE down-regulated the activity of CYP1A and up-regulated CYP3A activity （P 〈 0.05）. No impact of H-22 and BBSKE on CYP450 and CYP2E1 were found （P 〉0.05 ）. Conclusion： BBSKE showed an inhibition on CYP1A activity and an induction on CYP3A in H-22 tumor bearing mice and no effect on CYP2E1 were found.

关 键 词：乙烷硒啉 硫氧还原蛋白还原酶 细胞色素P450 

分 类 号：R979.1[医药卫生—药品] R994.2[医药卫生—药学]