Docosahexaenoic acid, G protein-coupled receptors, and melanoma: is G protein-coupled receptor 40 a potential therapeutic target?

J Surg Res. 2014 May 15;188(2):451-8. doi: 10.1016/j.jss.2014.01.037. Epub 2014 Jan 29.

Abstract

Background: To determine the effect of docosahexaenoic acid (DHA) on the growth of human melanoma in vitro and in vivo and to better understand the potential role of the G protein-coupled receptors (GPRs) in mediating this effect.

Materials and methods: For in vitro studies, human melanoma and control fibroblast cells were treated with DHA and TAK-875 (selective GPR40 agonist) and a cell viability assay was performed to determine cell counts. A murine subcutaneous xenograft model of human melanoma was used to test the effect of dietary treatment with an omega-3 fatty acid (FA) rich diet compared with an omega-6 FA rich diet on the growth of human melanoma in vivo. A similar animal model was used to test the effect of oral TAK-875 on the growth of established melanoma tumors in vivo.

Results: DHA has an inhibitory effect on the growth of human melanoma both in vitro and in vivo. Tumors from animals on the omega-3 FA rich diet were 69% smaller in weight (P = 0.005) and 76% smaller in volume compared with tumors from animals on the omega-6 FA rich diet. TAK-875 has an inhibitory effect on the growth of human melanoma both in vitro and in vivo. Tumors from animals treated with TAK-875 were 46% smaller in weight (P = 0.07), 62% smaller in volume (P = 0.03), and grew 77% slower (P = 0.04) compared with the placebo group.

Conclusions: DHA and TAK-875 have a profound and selective inhibitory effect on the growth of human melanoma both in vitro and in vivo.

Keywords: Docosahexaenoic acid; G protein–coupled receptor; GPR120; GPR40; Melanoma; Omega-3 fatty acid; Omega-3 polyunsaturated fatty acid.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzofurans / pharmacology
  • Benzofurans / therapeutic use*
  • Cell Line, Tumor
  • Docosahexaenoic Acids / pharmacology
  • Docosahexaenoic Acids / therapeutic use*
  • Humans
  • Melanoma, Experimental / diet therapy*
  • Melanoma, Experimental / drug therapy*
  • Melanoma, Experimental / metabolism
  • Mice
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / metabolism*
  • Sulfones / pharmacology
  • Sulfones / therapeutic use*
  • Xenograft Model Antitumor Assays

Substances

  • Benzofurans
  • FFAR1 protein, human
  • Receptors, G-Protein-Coupled
  • Sulfones
  • TAK-875
  • Docosahexaenoic Acids