Long-term administration of ranolazine attenuates diastolic dysfunction and adverse myocardial remodeling in a model of heart failure with preserved ejection fraction

Int J Cardiol. 2016 Aug 15:217:69-79. doi: 10.1016/j.ijcard.2016.04.168. Epub 2016 May 12.

Abstract

Background: To investigate the effects of chronic administration of ranolazine (RAN) on experimental model of heart failure with preserved ejection fraction.

Methods: Seven-weeks old Dahl salt-sensitive rats were fed a high salt diet for 5weeks to induce hypertension. Afterwards, rats continued with a high salt diet and were administered either with vehicle or RAN (20mg/kg/die, ip) for the following 8weeks. Control rats were maintained on a low salt diet.

Results: While systolic parameters were not altered, diastolic parameters were changed in high salt animals. Hemodynamic analysis showed a decreased dP/dt min, increased LVEDP, longer time constant and steeper slope of the end-diastolic pressure-volume relationship. Treatment with RAN attenuated these alterations and determined a reduction in mortality. Additionally, the magnitude of myocardial hypertrophy and activation of PI3K/Akt pathway were reduced. Alteration in diastolic compliance as a consequence of elevated myocardial stiffness was confirmed by an increase of collagen deposition and activation of pro-fibrotic TGF-β/SMAD3/CTGF signaling. These effects were counteracted by RAN. High salt rats had a decrease in SERCA2 and an increase in Na(+)/Ca(2+) exchanger (NCX). Treatment with RAN reduced NCX expression and determined an increment of SERCA2. Moreover, the levels of nitrotyrosine and oxidized dyhydroethidium were higher in high salt rats. RAN induced a decrement of oxidative stress, supporting the concept that reduction in ROS may mediate beneficial effects.

Conclusions: Our findings support the possibility that diastolic dysfunction can be attenuated by RAN, indicating its ability to affect active relaxation and passive diastolic compliance.

Keywords: Dahl salt-sensitive rats; Diastolic dysfunction; Heart failure with preserved ejection fraction; Ranolazine.

MeSH terms

  • Animals
  • Cardiovascular Agents / administration & dosage*
  • Disease Models, Animal
  • Drug Administration Schedule
  • Heart Failure / drug therapy*
  • Heart Failure / metabolism
  • Heart Failure / physiopathology
  • Humans
  • Hypertension / chemically induced
  • Hypertension / metabolism
  • Hypertension / physiopathology
  • Male
  • Phosphatidylinositol 3-Kinases / metabolism
  • Proto-Oncogene Proteins c-akt / metabolism
  • Ranolazine / administration & dosage*
  • Rats
  • Rats, Inbred Dahl
  • Signal Transduction / drug effects
  • Stroke Volume / drug effects*
  • Treatment Outcome
  • Ventricular Remodeling / drug effects*

Substances

  • Cardiovascular Agents
  • Ranolazine
  • Phosphatidylinositol 3-Kinases
  • Proto-Oncogene Proteins c-akt