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

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...