The Effect of Sorafenib, Tadalafil and Macitentan Treatments on Thyroxin-Induced Hemodynamic Changes and Cardiac Abnormalities

PLoS One. 2016 Apr 15;11(4):e0153694. doi: 10.1371/journal.pone.0153694. eCollection 2016.

Abstract

Multikinase inhibitors (e.g. Sorafenib), phosphodiesterase-5 inhibitors (e.g. Tadalafil), and endothelin-1 receptor blockers (e.g. Macitentan) exert influential protection in a variety of animal models of cardiomyopathy; however, their effects on thyroxin-induced cardiomyopathy have never been investigated. The goal of the present study was to assess the functional impact of these drugs on thyroxin-induced hemodynamic changes, cardiac hypertrophy and associated altered responses of the contractile myocardium both in-vivo at the whole heart level and ex-vivo at the cardiac tissue level. Control and thyroxin (500 μg/kg/day)-treated mice with or without 2-week treatments of sorafenib (10 mg/kg/day; I.P), tadalafil (1 mg/kg/day; I.P or 4 mg/kg/day; oral), macitentan (30 and 100 mg/kg/day; oral), and their vehicles were studied. Blood pressure, echocardiography and electrocardiogram were non-invasively evaluated, followed by ex-vivo assessments of isolated multicellular cardiac preparations. Thyroxin increased blood pressure, resulted in cardiac hypertrophy and left ventricular dysfunction in-vivo. Also, it caused contractile abnormalities in right ventricular papillary muscles ex-vivo. None of the drug treatments were able to significantly attenuate theses hemodynamic changes or cardiac abnormalities in thyroxin-treated mice. We show here for the first time that multikinase (raf1/b, VEGFR, PDGFR), phosphodiesterase-5, and endothelin-1 pathways have no major role in thyroxin-induced hemodynamic changes and cardiac abnormalities. In particular, our data show that the involvement of endothelin-1 pathway in thyroxine-induced cardiac hypertrophy/dysfunction seems to be model-dependent and should be carefully interpreted.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Pressure
  • Cardiomyopathies / drug therapy
  • Disease Models, Animal
  • Echocardiography
  • Electrocardiography
  • Heart Defects, Congenital / chemically induced
  • Heart Defects, Congenital / drug therapy*
  • Heart Rate
  • Hemodynamics
  • Male
  • Mice
  • Myocardial Contraction
  • Niacinamide / administration & dosage
  • Niacinamide / analogs & derivatives*
  • Organ Size
  • Phenylurea Compounds / administration & dosage*
  • Pyrimidines / administration & dosage*
  • Sorafenib
  • Sulfonamides / administration & dosage*
  • Tadalafil / administration & dosage*
  • Thyroxine / administration & dosage
  • Thyroxine / adverse effects*

Substances

  • Phenylurea Compounds
  • Pyrimidines
  • Sulfonamides
  • Niacinamide
  • Tadalafil
  • Sorafenib
  • Thyroxine
  • macitentan