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

胡陈; 于锋; 戴德哉; 戴茵

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

摘要

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ET_A和ET_B上调，且ET_B比ET_A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（10 μmol/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ET_A和ET_B过度表达有关。

Abstract: 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 ET_A and ET_B were increased by isoproterenol，in which the level of ET_Bwas higher than ET_A .This phenomenon was adjusted to different degrees by using propranolol，CPU86017 and RS chiral isomer in a dosage-relevant manner.The infervention effect of RS isomer was better than that of CPU86017 at the high dosage(10 μmol/L). Conclusion ：The cardiovascular effects of CPU86017 and RS chiral isomer could be correlative to the inhibition of the over-expressions of ET_Aand ET_B.

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