新型β_2受体激动剂川丁特罗对HepG2细胞中细胞色素P450 mRNA表达的影响  

Effect of novel β2 receptor agonist trantinterol on cytochrome P450 mRNA expression in HepG2 cells

作　　者：孙严彤[1,2] 郭颖杰[1] 张梦亮[1] 崔相勇[1] 顾景凯[1] 

机构地区：[1]吉林大学生命科学学院药物代谢研究中心,吉林长春130021 [2]吉林大学药学院药物分析教研室,吉林长春130021

出　　处：《吉林大学学报（医学版）》2010年第5期862-865,共4页Journal of Jilin University：Medicine Edition

基　　金：国家自然科学基金资助课题(30973587);"十一五"重大科技专项基金资助课题(2009ZX09304-003)

摘　　要：目的:研究新型β2受体激动剂川丁特罗(trantinterol)对细胞色素P450酶(CYP450)mRNA表达的影响,为临床合并用药提供理论依据。方法:人肝癌细胞(HepG2)中分别加入浓度为2.4、12、60、300、1200和4800ng·L-1的川丁特罗,MTT法检测药物作用下的细胞增殖。采用RT-PCR法检测HepG2细胞中CYP1A1、CYP2E1和CYP3A5亚型的mRNA表达量。结果:不同浓度的川丁特罗均未抑制HepG2细胞的增殖(P>0.05)。与对照组比较,川丁特罗给药组CYP3A5和CYP2E1mRNA表达无明显变化,而CYP1A1mRNA表达水平明显降低(P<0.01)。结论:川丁特罗能明显抑制HepG2细胞中CYP1A1mRNA表达,而对CYP3A5和CYP2E1表达无影响。Objective To study the effect of trantinterol,apotent and highly selective β2 receptor agonist,on the cytochrome P450 enzymes （CYP450）mRNA expression and provide a theoretical basis for clinical drug combination.Methods The cell proliferation of HepG2cells treated with 2.4,12,60,300,1 200and 4 800ng·L-1 trantinterol was analyzed by MTT.The mRNA expression levels of CYP1A1,CYP2E1and CYP3A5in HepG2cells were examined using the real-time quantitative reverse-transcriptase polymerase chain reaction in human hepatoma HepG2cells.Results Different concentrations of trantinterol didn＇t inhibit the proliferation of HepG2cells（P〉0.05）.Compared with control group,the mRNA expressions of CYP2E1and CYP3A5in trantinterol groups had no change,while the mRNA expression of CYP1A1was inhibited（P〈0.01）. Conclusion Exposure of HepG2cells to trantinterol has no effect on the mRNA expressions of CYP2E1and CYP3A5but inhibit the mRNA expression of CYP1A1.

关 键 词：川丁特罗 细胞色素P450 HEPG2细胞 实时定量PCR 

分 类 号：R969.1[医药卫生—药理学]