Nitric oxide-sensitive guanylyl cyclase stimulation improves experimental heart failure with preserved ejection fraction

JCI Insight. 2018 Feb 22;3(4):e96006. doi: 10.1172/jci.insight.96006.

Abstract

Heart failure with preserved ejection fraction (HFpEF) can arise from cardiac and vascular remodeling processes following long-lasting hypertension. Efficacy of common HF therapeutics is unsatisfactory in HFpEF. Evidence suggests that stimulators of the nitric oxide-sensitive soluble guanylyl cyclase (NOsGC) could be of use here. We aimed to characterize the complex cardiovascular effects of NOsGC stimulation using NO-independent stimulator BAY 41-8543 in a double-transgenic rat (dTGR) model of HFpEF. We show a drastically improved survival rate of treated dTGR. We observed less cardiac fibrosis, macrophage infiltration, and gap junction remodeling in treated dTGR. Microarray analysis revealed that treatment of dTGR corrected the dysregulateion of cardiac genes associated with fibrosis, inflammation, apoptosis, oxidative stress, and ion channel function toward an expression profile similar to healthy controls. Treatment reduced systemic blood pressure levels and improved endothelium-dependent vasorelaxation of resistance vessels. Further comprehensive in vivo phenotyping showed an improved diastolic cardiac function, improved hemodynamics, and less susceptibility to ventricular arrhythmias. Short-term BAY 41-8543 application in isolated untreated transgenic hearts with structural remodeling significantly reduced the occurrence of ventricular arrhythmias, suggesting a direct nongenomic role of NOsGC stimulation on excitation. Thus, NOsGC stimulation was highly effective in improving several HFpEF facets in this animal model, underscoring its potential value for patients.

Keywords: Cardiology; Heart failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Angiotensinogen / genetics
  • Animals
  • Arrhythmias, Cardiac / etiology
  • Arrhythmias, Cardiac / prevention & control*
  • Blood Pressure / drug effects
  • Chronic Disease / drug therapy
  • Disease Models, Animal
  • Drug Evaluation, Preclinical
  • Echocardiography
  • Heart Failure / complications
  • Heart Failure / drug therapy*
  • Heart Failure / genetics
  • Heart Failure / mortality
  • Heart Ventricles / diagnostic imaging
  • Heart Ventricles / drug effects
  • Heart Ventricles / physiopathology
  • Humans
  • Isolated Heart Preparation
  • Male
  • Morpholines / pharmacology
  • Morpholines / therapeutic use*
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use*
  • Rats
  • Rats, Transgenic
  • Renin / genetics
  • Soluble Guanylyl Cyclase / metabolism*
  • Stroke Volume / physiology
  • Survival Rate
  • Treatment Outcome

Substances

  • AGT protein, human
  • BAY 41-8543
  • Morpholines
  • Pyrimidines
  • Angiotensinogen
  • Renin
  • Soluble Guanylyl Cyclase

Grants and funding

The study was funded through a postdoc grant by Bayer AG (Wuppertal, Germany)