应激上调心肌内皮素受体和对氯苄基四氢小檗碱CPU86017及其RS异构体的干预作用  

Stress-up-regulated myocardial endothelin receptors are suppressed by chlorobenzyltetrahydroberberine CPU86017 and its RS chiral isomer

作　　者：胡陈[1] 于锋[1] 戴德哉[1] 戴茵[1] 

机构地区：[1]中国药科大学药理学研究室,南京210009

出　　处：《中国药科大学学报》2009年第4期374-379,共6页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.30572193)~~

摘　　要：目的:研究异丙肾上腺素诱导的心肌细胞中内皮素(ET)受体变化情况;研究对氯苄基四氢小檗碱CPU86017及其RS异构体对应激上调心肌内皮素受体的干预作用。方法:原代培养乳鼠心肌细胞,加入异丙肾上腺素造模,给予普萘洛尔、CPU86017及其RS异构体干预。结果:异丙肾上腺素同时诱导ETA和ETB上调,且ETB比ETA更明显。普萘洛尔、CPU86017及其RS异构进行干预后,均使ET受体异常表达改善,并呈剂量相关性。在高剂量(10μmol/L)下,RS异构体效应较CPU86017更显著。结论:CPU86017和RS异构体的心血管效应与其抑制ETA和ETB过度表达有关。Aim:To investigate the changes of endothelin(ET)receptors by isoproterenol in myocardial cells,and the invervention effects of CPU86017 and its RS isomer.Methods:Primary cultures of neonatal rat cardiomyocytes were prepared,and isoproterenol was added to each group for modeling,followed by drug interventions with propranolol,CPU86017 and RS chiral isomer respectively.Results:The expressions of ETA and ETB were increased by isoproterenol,in which the level of ETB was higher than ETA.This phenomenon was adjus...

关 键 词：异丙肾上腺素 氧化应激 ETA ETB 对氯苄基四氢小檗碱 CPU86017 手性异构体 

分 类 号：R965[医药卫生—药理学]