亚型选择性雌激素受体α和雌激素受体β激动剂在心血管系统中的功能作用及分子机制

Functional effects and molecular mechanisms of subtype-selective ERalpha and ERbeta agonists in the cardiovascular system.

作者信息

Arias-Loza P A, Jazbutyte V, Fritzemeier K H, Hegele-Hartung C, Neyses L, Ertl G, Pelzer T

机构信息

Medizinische Klinik I, University of Würzburg, Josef-Schneider Str. 2, 97080 Würzburg, Germany.

出版信息

Ernst Schering Found Symp Proc. 2006(1):87-106. doi: 10.1007/2789_2006_018.

DOI:10.1007/2789_2006_018

PMID:17824173

Abstract

Gender differences in the development of cardiovascular disease suggested for a protective function of estrogens in heart disease. The negative or neutral outcome of clinical trials on hormone replacement therapy provides clear evidence that the role of female sex hormones in the cardiovascular system is more complex than previously thought. In particular, the function of estrogens can not be understood without detailed knowledge on the specific function of both estrogen receptor subtypes in the heart and in the vasculature. In here, we review recent studies on subtype selective ERalpha and ERbeta agonists in different animal models of hypertension, cardiac hypertrophy and vascular inflammation. The results indicate that the activation of specific ER subtypes confers specific as well as redundant protective effects in hypertensive heart disease that might ultimately translate into novel treatment options for hypertensive heart disease.

摘要

心血管疾病发展中的性别差异表明雌激素对心脏病具有保护作用。激素替代疗法临床试验的阴性或中性结果清楚地证明，女性性激素在心血管系统中的作用比以前认为的更为复杂。特别是，如果没有关于雌激素受体两种亚型在心脏和血管系统中的具体功能的详细知识，就无法理解雌激素的功能。在此，我们综述了近期在高血压、心脏肥大和血管炎症等不同动物模型中关于亚型选择性雌激素受体α和雌激素受体β激动剂的研究。结果表明，特定雌激素受体亚型的激活在高血压性心脏病中具有特定的以及冗余的保护作用，这最终可能转化为高血压性心脏病的新治疗选择。