GW0742, a high-affinity PPAR -beta/delta agonist, inhibits acute lung injury in mice

Shock. 2010 Apr;33(4):426-35. doi: 10.1097/SHK.0b013e3181b8f2fb.

Abstract

Several lines of evidence suggest a biological role for peroxisome proliferator-activated receptor (PPAR) beta/delta in the pathogenesis of a number of diseases. The aim of this study was to investigate the effects of a high-affinity PPAR-beta/delta agonist, GW0742, in a mouse model of carrageenan (CAR)-induced pleurisy. Injection of CAR into the pleural cavity of mice elicited an acute inflammatory response characterized by accumulation of fluid containing a large number of neutrophils (polymorphonuclear leukocytes) in the pleural cavity, infiltration of polymorphonuclear leukocytes in lung tissues and subsequent lipid peroxidation, and increased production of nitrite/nitrate, TNF-alpha, and IL-1beta. Furthermore, CAR induced lung apoptosis (Bax and Bcl-2 expression), and nitrotyrosine formation was determined by immunohistochemical analysis of lung tissues. Administration of GW0742 (0.3 mg/kg, i.p. bolus) 30 min before and 30 min after a challenge with CAR caused a reduction in all the parameters of inflammation measured. Thus, based on these findings, we propose that a PPAR-beta/delta agonist such as GW0742 may be useful in the treatment of various inflammatory diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Lung Injury / prevention & control*
  • Animals
  • Apoptosis / drug effects
  • Carrageenan
  • I-kappa B Proteins / metabolism
  • Lipid Peroxidation / drug effects
  • Lung / drug effects
  • Lung / metabolism
  • Lung / pathology
  • Male
  • Mice
  • NF-KappaB Inhibitor alpha
  • Neutrophils / immunology
  • Nitric Oxide Synthase Type II / biosynthesis
  • PPAR delta / agonists
  • PPAR-beta / agonists
  • Pleurisy / chemically induced
  • Pleurisy / immunology
  • Pleurisy / pathology
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Thiazoles / therapeutic use*
  • Transcription Factor RelA / metabolism
  • Tumor Necrosis Factor-alpha / metabolism
  • Tyrosine / analogs & derivatives
  • Tyrosine / biosynthesis
  • bcl-2-Associated X Protein / metabolism

Substances

  • I-kappa B Proteins
  • Nfkbia protein, mouse
  • PPAR delta
  • PPAR-beta
  • Proto-Oncogene Proteins c-bcl-2
  • Thiazoles
  • Transcription Factor RelA
  • Tumor Necrosis Factor-alpha
  • bcl-2-Associated X Protein
  • NF-KappaB Inhibitor alpha
  • 3-nitrotyrosine
  • Tyrosine
  • (4-(((2-(3-fluoro-4-(trifluoromethyl)phenyl)-4-methyl-1,3-thiazol-5-yl)methyl)sulfanyl)-2-methylphenoxy)acetic acid
  • Carrageenan
  • Nitric Oxide Synthase Type II
  • Nos2 protein, mouse