Peroxisome proliferator-activated receptor gamma is required for the inhibitory effect of ciglitazone but not 15-deoxy-Delta 12,14-prostaglandin J2 on the NFkappaB pathway in human endothelial cells

Shock. 2007 Dec;28(6):722-726. doi: 10.1097/SHK.0b013e318055683a.

Abstract

Peroxisome proliferator-activated receptor gamma (PPARgamma) is a ligand-activated nuclear receptor with effects on inflammation, atherosclerosis, and apoptosis. The endogenous PPARgamma ligand, 15-deoxy-Delta12,14-PGJ2 (15d-PGJ2), and the synthetic ligand, ciglitazone, have anti-inflammatory properties in endothelial cells. In addition to PPARgamma-dependent effects on the anti-inflammatory process, it has been proposed that PPARgamma ligands may also inhibit the nuclear transcription factor kappaB (NFkappaB) pathway in a PPARgamma-independent manner. The purpose of this study was to compare the effects of 15d-PGJ2 and ciglitazone on the cytokine-induced activation of the NFkappaB pathway. Human umbilical vein endothelial cells (HUVECs) were transiently transfected with NFkappaB-luciferase or PPARgamma elements-luciferase reporter constructs for 48 h. The HUVECs were pretreated with 15d-PGJ2 or ciglitazone (30 microM) for 1 h, followed by a 4-h stimulation with tumor necrosis factor alpha (100 U/mL). Luciferase assay was performed to determine reporter activity. Additionally, HUVECs were transiently transfected with a dominant-negative mutant, which retains ligand and DNA binding but exhibits markedly reduced transactivation. Stimulation of HUVEC with tumor necrosis factor alpha increased NFkappaB activation while decreasing PPARgamma activity. Overexpression of a dominant-negative PPARgamma mutant prevented the inhibitory effect of ciglitazone on cytokine-induced NFkappaB activation in transfected human endothelial cells. Conversely, 15d-PGJ2 inhibited the cytokine-induced NFkappaB activation even in the absence of PPARgamma. Our data suggest that 15d-PGJ2 exerts direct inhibitory effects on the NFkappaB pathway through a PPARgamma-independent mechanism. On the contrary, the inhibitory effect of ciglitazone on the NFkappaB pathway seems to require PPARgamma activation.

Publication types

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

MeSH terms

  • Cells, Cultured
  • Cyclooxygenase 2 / metabolism
  • Dose-Response Relationship, Drug
  • E-Selectin / metabolism
  • Endothelial Cells / cytology
  • Endothelial Cells / drug effects*
  • Endothelial Cells / metabolism
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Intercellular Adhesion Molecule-1 / metabolism
  • Luciferases / genetics
  • Luciferases / metabolism
  • Mutation
  • NF-kappa B / genetics
  • NF-kappa B / metabolism*
  • PPAR gamma / genetics
  • PPAR gamma / metabolism*
  • Prostaglandin D2 / analogs & derivatives*
  • Prostaglandin D2 / pharmacology
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism
  • Signal Transduction / drug effects
  • Thiazolidinediones / pharmacology*
  • Transfection
  • Tumor Necrosis Factor-alpha / pharmacology
  • Vascular Cell Adhesion Molecule-1 / metabolism

Substances

  • 15-deoxy-delta(12,14)-prostaglandin J2
  • E-Selectin
  • NF-kappa B
  • PPAR gamma
  • Recombinant Fusion Proteins
  • Thiazolidinediones
  • Tumor Necrosis Factor-alpha
  • Vascular Cell Adhesion Molecule-1
  • Intercellular Adhesion Molecule-1
  • Luciferases
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin D2
  • ciglitazone