Antagonizing the CX3CR1 Receptor Markedly Reduces Development of Cardiac Hypertrophy After Transverse Aortic Constriction in Mice

J Cardiovasc Pharmacol. 2021 Dec 1;78(6):792-801. doi: 10.1097/FJC.0000000000001130.

Abstract

Left-ventricular hypertrophy, characterized by cardiomyocyte hypertrophy, interstitial cell proliferation, and immune cell infiltration, is a high risk factor for heart failure and death. Chemokines interacting with G protein-coupled chemokine receptors probably play a role in left-ventricular hypertrophy development by promoting recruitment of activated leukocytes and modulating left-ventricular remodeling. Using the minimally invasive model of transverse aortic constriction in mice, we demonstrated that a variety of chemokine and chemokine receptor messenger Ribonucleic Acid are overexpressed in the early and late phase of hypertrophy progression. Among the chemokine receptors, Cx3cr1 and Ccr2 were most strongly overexpressed and were significantly upregulated at 3, 7, and 14 days after transverse aortic constriction. Ligands of CX3CR1 (Cx3cl1) and CCR2 (Ccl2, Ccl7, Ccl12) were significantly overexpressed in the left ventricle at the early stages after mechanical pressure overload. Pharmacological inhibition of CX3CR1 signaling using the antagonist AZD8797 led to a significant reduction of hypertrophy, whereas inhibition of CCR2 with the RS504393 antagonist did not show any effect. Furthermore, AZD8797 treatment reduced the expression of the hypertrophic marker genes Nppa and Nppb as well as the profibrotic genes Tgfb1 and Col1a1 at 14 days after transverse aortic constriction. These findings strongly suggest the involvement of the CX3CR1/CX3CL1 pathway in the pathogenesis of left-ventricular hypertrophy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta / physiopathology
  • Aorta / surgery
  • Atrial Natriuretic Factor / genetics
  • Atrial Natriuretic Factor / metabolism
  • CX3C Chemokine Receptor 1 / antagonists & inhibitors*
  • CX3C Chemokine Receptor 1 / genetics
  • CX3C Chemokine Receptor 1 / metabolism
  • Chemokine CX3CL1 / genetics
  • Chemokine CX3CL1 / metabolism
  • Collagen Type I, alpha 1 Chain / genetics
  • Collagen Type I, alpha 1 Chain / metabolism
  • Constriction
  • Disease Models, Animal
  • Fibrosis
  • Hypertrophy, Left Ventricular / etiology
  • Hypertrophy, Left Ventricular / metabolism
  • Hypertrophy, Left Ventricular / physiopathology
  • Hypertrophy, Left Ventricular / prevention & control*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Myocytes, Cardiac / drug effects*
  • Myocytes, Cardiac / metabolism
  • Myocytes, Cardiac / pathology
  • Natriuretic Peptide, Brain / genetics
  • Natriuretic Peptide, Brain / metabolism
  • Pyrimidines / pharmacology*
  • Signal Transduction
  • Thiazoles / pharmacology*
  • Time Factors
  • Transforming Growth Factor beta1 / genetics
  • Transforming Growth Factor beta1 / metabolism
  • Ventricular Function, Left / drug effects*
  • Ventricular Remodeling / drug effects*

Substances

  • AZD8797
  • CX3C Chemokine Receptor 1
  • Chemokine CX3CL1
  • Col1a1 protein, mouse
  • Collagen Type I, alpha 1 Chain
  • Cx3cl1 protein, mouse
  • Cx3cr1 protein, mouse
  • Nppa protein, mouse
  • Pyrimidines
  • Tgfb1 protein, mouse
  • Thiazoles
  • Transforming Growth Factor beta1
  • Natriuretic Peptide, Brain
  • Atrial Natriuretic Factor