GPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effects

Cell. 2010 Sep 3;142(5):687-98. doi: 10.1016/j.cell.2010.07.041.

Abstract

Omega-3 fatty acids (omega-3 FAs), DHA and EPA, exert anti-inflammatory effects, but the mechanisms are poorly understood. Here, we show that the G protein-coupled receptor 120 (GPR120) functions as an omega-3 FA receptor/sensor. Stimulation of GPR120 with omega-3 FAs or a chemical agonist causes broad anti-inflammatory effects in monocytic RAW 264.7 cells and in primary intraperitoneal macrophages. All of these effects are abrogated by GPR120 knockdown. Since chronic macrophage-mediated tissue inflammation is a key mechanism for insulin resistance in obesity, we fed obese WT and GPR120 knockout mice a high-fat diet with or without omega-3 FA supplementation. The omega-3 FA treatment inhibited inflammation and enhanced systemic insulin sensitivity in WT mice, but was without effect in GPR120 knockout mice. In conclusion, GPR120 is a functional omega-3 FA receptor/sensor and mediates potent insulin sensitizing and antidiabetic effects in vivo by repressing macrophage-induced tissue inflammation.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • 3T3-L1 Cells
  • Animals
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / metabolism
  • Cell Line
  • Dietary Fats / metabolism
  • Dietary Supplements
  • Fatty Acids, Omega-3 / administration & dosage*
  • Fatty Acids, Omega-3 / metabolism*
  • Humans
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / metabolism
  • Insulin Resistance*
  • Macrophages / immunology
  • Mice
  • Mice, Knockout
  • Obesity / complications
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*

Substances

  • Anti-Inflammatory Agents
  • Dietary Fats
  • FFAR4 protein, mouse
  • Fatty Acids, Omega-3
  • Hypoglycemic Agents
  • Receptors, G-Protein-Coupled