Cardioprotection of 17β-estradiol against hypoxia/reoxygenation in cardiomyocytes is partly through up-regulation of CRH receptor type 2

Mol Cell Endocrinol. 2014 Jan 25;382(1):17-25. doi: 10.1016/j.mce.2013.09.002. Epub 2013 Sep 11.

Abstract

Estrogens have been suggested to exert cardioprotection through maintaining endogenous cardioprotective mechanisms. In the present study, we investigated whether estrogens protect cardiomyocytes against hypoxia/reoxygenation (H/R) via modulating urocortins (UCNs) and their receptor corticotrophin-releasing hormone receptor type 2 (CRHR2). We found that 17β-estradiol (E2) enhanced UCN cardioprotection against H/R and increased CRHR2 expression in neonatal rat cardiomyocytes. E2 protected cardiomyocytes against H/R, which was impaired by CRHR2 antagonist or knockdown of CRHR2. Estrogen receptor α (ERα) antagonist treatment or ERα knockdown could abolish E2-induced CRHR2 up-regulation. Moreover, knockdown of Sp1 also attenuated E2-induced CRHR2 up-regulation. Ovariectomy resulted in down-regulation of CRHR2 and Sp-1 in myocardium of mice, which was restored by E2 or ERα agonist treatment. These results suggest that estrogens act on ERα to up-regulate CRHR2 expression in cardiomyocytes, thereby enhancing cardioprotection of UCNs against H/R.

Keywords: 17β-estradiol; CRHR2; Cardiomyocytes; Corticotropin-releasing hormone receptor type 2; E2; ER; EREs; Estrogens; H/R; Hypoxia/reoxygenation; IHD; IPC; LDH; Lactate Dehydrogenase; MTT; RIA; Radioimmunoassay; Sp1; Specific protein1; UCN; Urocortins; corticotrophin-releasing hormone receptor type 2; estrogen receptor; estrogen responses elements; hypoxia/reoxygenation; ischemic heart disease; ischemic preconditioning; methyl thiazolyl tetrazolium; siRNA; small interfering RNA; specific protein 1; urocortin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cardiotonic Agents / pharmacology*
  • Cell Hypoxia / drug effects
  • Down-Regulation / drug effects
  • Estradiol / pharmacology*
  • Estrogen Receptor alpha / agonists
  • Estrogen Receptor alpha / metabolism
  • Female
  • Gene Knockdown Techniques
  • Mice
  • Myocardium / metabolism
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism*
  • Ovariectomy
  • Oxygen / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors
  • Receptors, Corticotropin-Releasing Hormone / metabolism*
  • Sp1 Transcription Factor / metabolism
  • Up-Regulation / drug effects*
  • Urocortins / pharmacology

Substances

  • CRF receptor type 2
  • Cardiotonic Agents
  • Estrogen Receptor alpha
  • Receptors, Corticotropin-Releasing Hormone
  • Sp1 Transcription Factor
  • Urocortins
  • Estradiol
  • Oxygen