Suberoylanilide hydroxamic acid: a potential epigenetic therapeutic agent for lung fibrosis?

Eur Respir J. 2009 Jul;34(1):145-55. doi: 10.1183/09031936.00084808.

Abstract

Pulmonary fibrosis represents a fatal stage of interstitial lung diseases of known and idiopathic aetiology. No effective therapy is currently available. Based on an indication-discovery approach we present novel in vitro evidence that the histone deacetylases inhibitor suberoylanilide hydroxamic acid (SAHA), an FDA approved anti-cancer drug, has antifibrotic and anti-inflammatory potential. Human lung fibroblasts (fetal, adult and idiopathic adult pulmonary fibrosis) were treated with transforming growth factor (TGF)-beta 1 with or without SAHA. Collagen deposition, alpha-smooth muscle actin (alpha-SMA) expression, matrix metalloproteinase (MMP)1 activity, tissue inhibitor of MMP (TIMP)1 production, apoptosis and cell proliferation were assessed. Pro-inflammatory cytokines relevant to pulmonary fibrosis were assayed in SAHA-treated human peripheral blood mononuclear cells (PBMC) and its subpopulations. SAHA abrogated TGF-beta 1 effects on all the fibroblast lines by preventing their transdifferentiation into alpha-SMA positive myofibroblasts and increased collagen deposition without inducing apoptosis. However, MMP1 activity and TIMP1 production was modulated without a clear fibrolytic effect. SAHA also inhibited serum-induced proliferation of the fibroblast lines and caused hyperacetylation of alpha-tubulin and histone. Cytokine secretion was inhibited from PBMC and lymphocytes at nonapoptotic concentrations. Taken together, these data demonstrate combined antifibrotic and anti-inflammatory properties of SAHA, suggesting its therapeutic potential for pulmonary fibrosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / metabolism
  • Anti-Inflammatory Agents / pharmacology
  • Cell Line
  • Cell Proliferation
  • Collagen / metabolism
  • Epigenesis, Genetic*
  • Fibroblasts / drug effects
  • Fibrosis / drug therapy*
  • Fibrosis / genetics*
  • Humans
  • Hydroxamic Acids / therapeutic use*
  • Immunohistochemistry / methods
  • Lung / drug effects
  • Lung / pathology*
  • Matrix Metalloproteinase 1 / metabolism
  • Muscle, Smooth / metabolism
  • Tissue Inhibitor of Metalloproteinase-1 / biosynthesis
  • Vorinostat

Substances

  • Actins
  • Anti-Inflammatory Agents
  • Hydroxamic Acids
  • Tissue Inhibitor of Metalloproteinase-1
  • Vorinostat
  • Collagen
  • Matrix Metalloproteinase 1