Inhibition of farnesyl pyrophosphate synthase prevents angiotensin II-induced cardiac fibrosis in vitro

Clin Exp Immunol. 2014 Jun;176(3):429-37. doi: 10.1111/cei.12282.

Abstract

Farnesyl pyrophosphate synthase (FPPS)-catalysed isoprenoid intermediates are important for the activation of Ras homologue gene family, member A (RhoA) in angiotensin (Ang) II-induced cardiac fibrosis. This study was designed to investigate the specific role of FPPS in the development of cardiac fibrosis. We demonstrated that FPPS expression was elevated in both in-vivo and in-vitro models of Ang II-mediated cardiac fibrosis. FPPS inhibition by zolendronate and FPPS knock-down by a silencing lentivirus decreased the expression of cardiac fibrosis marker genes, including collagen I, collagen III and transforming growth factor (TGF)-β1. FPPS inhibition was reversed by geranylgeraniol (GGOH) and mimicked by RhoA knock-down with siRhoA. The antagonistic effect of GGOH on the zolendronate-mediated modulation of RhoA activation in Ang II-stimulated cardiac fibroblasts was demonstrated by a pull-down assay. Furthermore, FPPS knock-down also prevented RhoA activation by Ang II in vitro. In conclusion, FPPS and RhoA may be part of a signalling pathway that plays an important role in Ang II-induced cardiac fibrosis in vitro.

Keywords: RhoA; cardiac fibrosis; farnesyl pyrophosphate synthase.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Angiotensin II / adverse effects
  • Animals
  • Collagen Type I / genetics
  • Collagen Type I / metabolism
  • Collagen Type III / genetics
  • Collagen Type III / metabolism
  • Disease Models, Animal
  • Enzyme Activation
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Fibrosis / chemically induced
  • Gene Expression
  • Gene Knockout Techniques
  • Geranyltranstransferase / genetics*
  • Geranyltranstransferase / metabolism
  • Myocardium / metabolism*
  • Myocardium / pathology*
  • Protein Prenylation
  • RNA Interference
  • Rats
  • Transforming Growth Factor beta1 / genetics
  • Transforming Growth Factor beta1 / metabolism
  • rhoA GTP-Binding Protein / genetics
  • rhoA GTP-Binding Protein / metabolism

Substances

  • Collagen Type I
  • Collagen Type III
  • Transforming Growth Factor beta1
  • Angiotensin II
  • Geranyltranstransferase
  • rhoA GTP-Binding Protein