Effect of novel agonist of soluble guanylate cyclase sGC 003 on endothelin-1-induced cardiomyocyte hypertrophy
10.3867/j.issn.1000-3002.2016.04.006
- VernacularTitle:新型可溶性鸟苷酸环化酶激动剂sGC003对内皮素诱导的心肌细胞肥大的作用
- Author:
Ke LIU
;
Lingdi YAN
;
Zheng YONG
;
Zehui GONG
;
Ruibin SU
- Publication Type:Journal Article
- Keywords:
soluble guanylate cyclase;
agonist;
sGC003;
cardiomyocytes;
endothelin-1;
cardiac hypertrophy
- From:
Chinese Journal of Pharmacology and Toxicology
2016;30(4):338-343
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE To investigate the protective effect of sGC003,a novel agonist of soluble guanylate cyclase,on endothelin-1(ET-1)-induced cardiomyocyte hypertrophy. METHODS Cardiomy?ocytes were isolated from neonatal Sprague-Dawley rats using serial enzymatic digestion and then incubated with ET-1 10 nmol·L-1 in the absence or presence of sGC003 0.01,0.1 and 1.0μmol·L-1. Hyper?trophic responses including the cardiomyocyte area(Image-Pro Plus 6.0),the expression of atrial natri?uretic peptide gene(ANP)mRNA(RT-PCR method)and total protein content(BCA method)were detect?ed. RESULTS After 48 h stimulation with ET-1 10 nmol·L-1,the cardiomyocyte area increased by 80%(P<0.01),the total protein content increased by 120%(P<0.01) and the expression of ANP mRNA up-regulated by 140%(P<0.01). sGC003 0.01,0.1 and 1.0μmol · L-1 elicited antihypertrophic actions, including inhibition of ET-1-mediated increase in the cardiomyocyte area(P<0.01),raised total protein content(P<0.05)and upregulation of ANP mRNA(P<0.05). CONCLUSION sGC003 has protective,car?diomyocyte-selective antihypertrophic effects in vitro.
