Stress-up-regulated myocardial endothelin receptors are suppressed by chlo-robenzyltetrahydroberberine CPU86017 and its RS chiral isomer
10.3321/j.issn:1000-5048.2009.04.017
- VernacularTitle: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
- Author:
Chen HU
;
Feng YU
;
Dezai DAI
;
Yin DAI
- Publication Type:Journal Article
- Keywords:
isoproterenol;
oxidative stress;
ET_A;
ET_B;
chlorobenzyltetrahydroberberine;
CPU86017;
chiral isomer
- From:
Journal of China Pharmaceutical University
2009;40(4):374-379
- CountryChina
- Language:Chinese
-
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 cardiomyo-cytes 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_B was 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_A and ET_B.
