15-lipoxygenase-1 metabolites down-regulate peroxisome proliferator-activated receptor gamma via the MAPK signaling pathway

J Biol Chem. 2001 Sep 14;276(37):34545-52. doi: 10.1074/jbc.M100280200. Epub 2001 Jul 10.

Abstract

Human colon tumors have elevated levels of 15-lipoxygenase-1 (15-LO-1), suggesting that 15-LO-1 may play a role in the development of colorectal cancer. Also, 15-LO-1 metabolites can up-regulate epidermal growth factor signaling pathways, which results in an increase in mitogenesis. However, metabolites of 15-LO-1 can serve as ligands for peroxisome proliferator-activated receptor gamma (PPARgamma), and activation of this receptor causes most colon cancer cell lines to undergo a differentiative response and reverse their malignant phenotype. Hence, the role 15-LO-1 plays in colon cancer is not clear. To clarify the role of 15-LO-1 in carcinogenesis, the effect of 15-LO-1 and its metabolites on epidermal growth factor signaling and PPARgamma was investigated. In HCT-116 cells, exogenously added 15-LO-1 metabolites, 13-(S)-hydroxyoctadecadienoic acid, 13-(R)-hydroxyoctadecadienoic acid, and 13-(S)-hydroperoxyoctadecadienoic acid, up-regulated the MAPK signaling pathway, and an increase in PPARgamma phosphorylation was observed. Furthermore, in stable overexpressing 15-LO-1 HCT-116 cells, which produce endogenous 15-LO-1 metabolites, an up-regulation in mitogen-activated protein kinase and PPARgamma phosphorylation was observed. Incubation with a MAPK inhibitor ablated MAPK and PPARgamma phosphorylation. The 15-LO-1 up-regulates MAPK activity and increases PPARgamma phosphorylation, resulting in a down-regulation of PPARgamma activity. Thus, 15-LO-1 metabolites may not only serve as ligands for PPARgamma but can down-regulate PPARgamma activity via the MAPK signaling pathway.

MeSH terms

  • Arachidonate 15-Lipoxygenase / physiology*
  • Colonic Neoplasms / enzymology
  • Colonic Neoplasms / etiology
  • Dose-Response Relationship, Drug
  • Down-Regulation
  • Humans
  • Isoenzymes / physiology*
  • Linoleic Acids / pharmacology
  • MAP Kinase Signaling System*
  • Phosphorylation
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Transcription Factors / metabolism*
  • Tumor Cells, Cultured

Substances

  • Isoenzymes
  • Linoleic Acids
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors
  • 13-hydroxy-9,11-octadecadienoic acid
  • Arachidonate 15-Lipoxygenase