Sacubitril/valsartan improves diastolic left ventricular stiffness with increased titin phosphorylation via cGMP-PKG activation in diabetic mice

Sci Rep. 2024 Oct 23;14(1):25081. doi: 10.1038/s41598-024-75757-8.

Abstract

Titin, a giant sarcomeric protein, regulates diastolic left ventricular (LV) passive stiffness as a molecular spring and could be a therapeutic target for diastolic dysfunction. Sacubitril/valsartan (Sac/Val), an angiotensin receptor neprilysin inhibitor, has been shown to benefit patients with heart failure with preserved ejection fraction. The effect of Sac/Val is thought to be due to the enhancement of the cGMP/PKG pathway via natriuretic peptide. In this study, the effects of Sac/Val on LV diastolic dysfunction are demonstrated in a mouse diabetic cardiomyopathy model focusing on titin phosphorylation. Sac/Val-treated diabetic mice showed a greater increase in myocardial levels of cGMP-PKG than Val-treated and control mice. Conductance catheter analysis showed a significant reduction in LV stiffness in diabetic mice, but not in non-diabetic mice. Notably, diastolic LV stiffness was significantly reduced in Sac/Val-treated diabetic hearts compared with Val-treated or vehicle-treated diabetic mice. The phosphorylation level of titin (N2B), which determines passive stiffness and modulates active contraction, was higher in Sac/Val-treated hearts compared with Val-treated hearts in diabetic mice. Given that alteration of titin phosphorylation through PKG contributes to myocardial stiffness, the beneficial effects of Sac/Val in heart failure might be partly attributed to the induction of titin phosphorylation.

Keywords: Cardiomyopathy; Diabetes; Diastolic dysfunction; HFpEF; Myocardial stiffness; Titin.

MeSH terms

  • Aminobutyrates* / pharmacology
  • Angiotensin Receptor Antagonists / pharmacology
  • Animals
  • Biphenyl Compounds* / pharmacology
  • Biphenyl Compounds* / therapeutic use
  • Connectin* / metabolism
  • Cyclic GMP* / metabolism
  • Cyclic GMP-Dependent Protein Kinases* / metabolism
  • Diabetes Mellitus, Experimental* / drug therapy
  • Diabetes Mellitus, Experimental* / metabolism
  • Diabetes Mellitus, Experimental* / physiopathology
  • Diabetic Cardiomyopathies / drug therapy
  • Diabetic Cardiomyopathies / metabolism
  • Diabetic Cardiomyopathies / physiopathology
  • Diastole / drug effects
  • Drug Combinations*
  • Heart Ventricles / drug effects
  • Heart Ventricles / metabolism
  • Heart Ventricles / physiopathology
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Phosphorylation / drug effects
  • Protein Kinases
  • Valsartan* / pharmacology
  • Ventricular Dysfunction, Left / drug therapy
  • Ventricular Dysfunction, Left / etiology
  • Ventricular Dysfunction, Left / metabolism

Substances

  • Valsartan
  • Connectin
  • Cyclic GMP-Dependent Protein Kinases
  • Drug Combinations
  • Biphenyl Compounds
  • Cyclic GMP
  • sacubitril and valsartan sodium hydrate drug combination
  • Aminobutyrates
  • titin protein, mouse
  • Angiotensin Receptor Antagonists
  • Protein Kinases