In search of pulmonary hypertension treatments: Effect of 17β-estradiol on PGI2 pathway in human pulmonary artery

Prostaglandins Leukot Essent Fatty Acids. 2021 Sep:172:102321. doi: 10.1016/j.plefa.2021.102321. Epub 2021 Aug 9.

Abstract

Introduction: Prostacyclin (PGI2) is synthetized by PGI2 synthase (PGIS) and induces vasorelaxation via activation of cyclic AMP (cAMP) generating IP-receptor. Several components of the PGI2 signaling pathway are reduced in patients with pulmonary hypertension (PH).

Aim: To study the effect of 17β-estradiol (E2) on the PGI2 signaling pathway in human pulmonary arteries (HPA) and in their smooth muscle cells (hPASMC) derived from Group-3 PH and non-PH patients.

Methods: Following E2-treatments of isolated HPA and cultured hPASMC, we measured: 6-keto-Prostaglandin F (PGI2 stable metabolite) by ELISA, PGIS and IP protein levels by Western blot and HPA vasorelaxations with an organ bath system.

Results: Incubation with E2 (24/48 h, doses ≥ 10 nM) significantly increased the expression of PGIS in hPASMC derived from both PH (65-98%) and non-PH (21-33%) patients, whereas incubation with E2 (2 h, 0.1 and 1 µM) increased 6-keto-PGF production in HPA from Group-3 PH patients only, and did not affect 6-keto-PGF production in hPASMC from either non-PH or Group-3 PH patients. Increases in IP receptor expression were observed following 10 mM E2-treatment of hPASMC from non-PH (33% after 48 h) and Group-3 PH (23% after 24 h) patient lungs. Finally, preincubation with 100 nM E2 significantly increased arachidonic acid-induced vasorelaxation of HPA from non-PH patient lungs but not of HPA from Group-3 PH patient lungs.

Conclusion: E2-treatment may help to restore the PGI2-pathway in Group-3 PH.

Keywords: 17β-estradiol; Human pulmonary artery; Human pulmonary artery smooth muscle cells; PGI(2); Pulmonary hypertension.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 6-Ketoprostaglandin F1 alpha / metabolism*
  • Antihypertensive Agents / pharmacology
  • Arachidonic Acid / pharmacology
  • Case-Control Studies
  • Cytochrome P-450 Enzyme System / drug effects*
  • Cytochrome P-450 Enzyme System / metabolism
  • Endothelial Cells / drug effects
  • Endothelial Cells / metabolism
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / metabolism
  • Endothelium, Vascular / physiopathology
  • Epoprostenol / analogs & derivatives
  • Epoprostenol / pharmacology
  • Estradiol / pharmacology*
  • Estrogens / pharmacology*
  • Female
  • Humans
  • Hypertension, Pulmonary / metabolism*
  • Hypertension, Pulmonary / physiopathology
  • Intramolecular Oxidoreductases / drug effects*
  • Intramolecular Oxidoreductases / metabolism
  • Male
  • Middle Aged
  • Muscle, Smooth, Vascular / cytology
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Muscle, Smooth, Vascular / physiopathology
  • Myocytes, Smooth Muscle / drug effects*
  • Myocytes, Smooth Muscle / metabolism
  • Pulmonary Artery / cytology
  • Pulmonary Artery / drug effects*
  • Pulmonary Artery / metabolism
  • Pulmonary Artery / physiopathology
  • Vasodilation / drug effects*

Substances

  • Antihypertensive Agents
  • Estrogens
  • Arachidonic Acid
  • Estradiol
  • 6-Ketoprostaglandin F1 alpha
  • Cytochrome P-450 Enzyme System
  • Epoprostenol
  • Intramolecular Oxidoreductases
  • prostacyclin synthetase
  • treprostinil