槟榔碱对大鼠肝脏CYP2E1的体内诱导作用  

Induction of rat hepatic CYP2E1 expression by arecoline in vivo

作　　者：黄祥涛 肖润梅[1] 王明凤[1] 王俊俊[1] 陈勇[1] 

机构地区：[1]湖北大学中药生物技术省重点实验室,湖北大学生物资源绿色转化协同创新中心,湖北武汉430062

出　　处：《药学学报》2016年第1期153-156,共4页Acta Pharmaceutica Sinica

摘　　要：槟榔或槟榔果实,是广泛使用的嗜好品。研究表明,槟榔咀嚼物的使用与口腔癌、肥胖、糖尿病、高血压、高脂血症、肝硬化和肝细胞癌等相关。槟榔碱（图1）是槟榔所含的主要生物碱,对肝细胞有毒性,且巯基消耗及活性氧（reactive oxygen species,ROS）攻击是槟榔碱所致肝损伤的主要原因）。The regulation mechanism of arecoline on rat hepatic CYP2E1 was studied in vivo. After oral administration of arecoline hydrobromide（AH; 4, 20 and 100 mg·kg^-1·d^-1） to rats for one week, the hepatic CYP2E1 m RNA level remained unchanged, but the hepatic CYP2E1 protein content was dose-dependently increased. Additionally, although the hepatic CYP2E1 activity was induced by AH treatment, the induction was attenuated with the increase in dosage. The results indicate that the effect of arecoline on rat hepatic CYP2 El does not involve transcriptional activation of the gene, but largely involves the stabilization of CYP2E1 protein against degradation or increased efficiency of CYP2E1 m RNA translation, and additionally involve the post- translational modification of CYP2E1 protein. Furthermore, the CYP2E1 response is fairly equal among the different species, the induction of rat hepatic CYP2E1 by arecoline suggests that there is a risk of metabolic interaction among the substrate drugs of CYP2E1 in betel-quid use human.

关 键 词：槟榔碱 CYP2E1 诱导作用 

分 类 号：R969[医药卫生—药理学]