地非三唑对大鼠肝细胞细胞色素P450 CYP1A1/2的诱导作用  

Inductive effect of diphenytriazol on hepatic cytochrome P-450 CYP1A1/2 of rats

作　　者：陈琳[1] 阮昊[1] 姚彤炜[1] 

机构地区：[1]浙江大学药学院药物分析和药物代谢研究室,浙江杭州310058

出　　处：《中国药理学与毒理学杂志》2007年第6期501-504,共4页Chinese Journal of Pharmacology and Toxicology

摘　　要：目的试从mRNA表达水平阐明地非三唑对鼠肝微粒体中细胞色素P450 CYP1A1/2的诱导机制。方法给SD大鼠腹腔注射地非三唑,采用Tr-izol法提取大鼠肝脏RNA,用RT-PCR测定经地非三唑处理1,2及4d的鼠肝中细胞色素P450 CYP1A1,CYP1A2 mRNA的表达水平。结果地非三唑处理不同时间的鼠肝细胞中细胞色素P450CYP1A1,CYP1A2 mRNA的表达水平比空白对照组明显增加,空白对照组CYP1A1吸光度比值为0.270±0.040,诱导1,2及4d的吸光度比值分别为0.343±0.055,0.417±0.045及0.603±0.083;空白对照组的CYP1A2吸光度比值为0.613±0.189,而诱导1,2及4d的吸光度比值分别为1.510±0.226,3.057±0.518及4.120±0.458。随着诱导时间的增加,细胞色素P450 CYP1A1及CYP1A2 mRNA的表达也逐步增加,诱导时间与表达水平之间存在一定的线性关系,相关系数分别为0.9984和0.9563。结论地非三唑对细胞色素P450 CYP1A1/2 mRNA表达具有诱导作用。AIM To investigate the mechanism involved in the induction effort of diphenytriazol on rat hepatic cytochrome P-450 CYP1A1/2 enzymes. METHODS SpragueDawley rats were pretreated intraperitoneally with the same daily dose of diphenytriazol for different days. The mRNA level of cytochrome P-450 CYP1A1/CYP1 A2 in diphenytriazol pretreated rats liver was evaluated by RT-PCR. RESULTS Both of the expression levels of cytochrome P-450 CYP1 A1 and CYP1A2 mRNA were significantly improved. For cytochrome P-450 CYP13.1 mRNA, the control group was 0.270 ±0. 040, and diphenytriazol treated for 1, 2 and 4 d groups were 0.343 ±0.055, 0.417 ±0.045 and 0.603 ±0.083, respectively; for CYP1 A2 mRNA, the control group was 0. 613 ± 0. 189, and diphenytriazol treated for 1, 2 and 4 d groups were 1. 510 ± 0.226, 3.057±0.518 and4. 120 ±0.458, respectively. The correlation coefficient between the expression level of target mRNA and the treatment time were 0. 9984 and 0. 9563, respectively. CONCLUSION Diphenytriazol has inductive effect on expressions of rat hepat- ic eytoehrome P-450 CYP1A1/2.

关 键 词：地非三唑 细胞色素P450 CYP1A1 细胞 色素P450 CYP1A2 

分 类 号：R96[医药卫生—药理学]