Peroxisome proliferator-activated receptor δ agonist attenuates hepatic steatosis by anti-inflammatory mechanism

Exp Mol Med. 2012 Oct 31;44(10):578-85. doi: 10.3858/emm.2012.44.10.066.

Abstract

Although peroxisome proliferator receptor (PPAR)-α and PPAR-γ agonist have been developed as chemical tools to uncover biological roles for the PPARs such as lipid and carbohydrate metabolism, PPAR-δ has not been fully investigated. In this study, we examined the effects of the PPAR-δ agonist GW0742 on fatty liver changes and inflammatory markers. We investigated the effects of PPAR-δ agonist GW0742 on fatty liver changes in OLETF rats. Intrahepatic triglyceride contents and expression of inflammatory cytokines such as tumor necrosis factor-α (TNF-α) and monocyte chemo-attractant protein-1 (MCP-1) and also, PPAR-γ coactivator (PGC)-1α gene were evaluated in liver tissues of OLETF rats and HepG2 cells after GW0742 treatment. The level of TNF-α and MCP-1 was also examined in supernatant of Raw264. 7 cell culture. To address the effects of GW0742 on insulin signaling, we performed in vitro study with AML12 mouse hepatocytes. Rats treated with GW0742 (10 mg/kg/day) from 26 to 36 weeks showed improvement in fatty infiltration of the liver. In liver tissues, mRNA expressions of TNF-α, MCP-1, and PGC-1α were significantly decreased in diabetic rats treated with GW0742 compared to diabetic control rats. We also observed that GW0742 had inhibitory effects on palmitic acid-induced fatty accumulation and inflammatory markers in HepG2 and Raw264.7 cells. The expression level of Akt and IRS-1 was significantly increased by treatment with GW0742. The PPAR-δ agonist may attenuate hepatic fat accumulation through anti-inflammatory mechanism, reducing hepatic PGC-1α gene expression, and improvement of insulin signaling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / therapeutic use
  • Blood Glucose
  • Cytokines / genetics
  • Cytokines / metabolism
  • Diabetes Mellitus / blood
  • Diabetes Mellitus / immunology
  • Diabetes Mellitus / metabolism
  • Fatty Liver / blood
  • Fatty Liver / drug therapy*
  • Fatty Liver / immunology
  • Glucose Tolerance Test
  • Hep G2 Cells
  • Humans
  • Insulin Resistance
  • Liver / metabolism
  • Male
  • PPAR delta / agonists*
  • PPAR delta / metabolism
  • Rats
  • Rats, Long-Evans
  • Thiazoles / pharmacology*
  • Thiazoles / therapeutic use
  • Triglycerides / metabolism

Substances

  • Anti-Inflammatory Agents
  • Blood Glucose
  • Cytokines
  • PPAR delta
  • Thiazoles
  • Triglycerides
  • (4-(((2-(3-fluoro-4-(trifluoromethyl)phenyl)-4-methyl-1,3-thiazol-5-yl)methyl)sulfanyl)-2-methylphenoxy)acetic acid