Feedback control of cyclooxygenase-2 expression through PPARgamma

J Biol Chem. 2000 Sep 8;275(36):28028-32. doi: 10.1074/jbc.M001387200.

Abstract

Cyclooxygenase-2 (COX-2), a rate-limiting enzyme for prostaglandins (PG), plays a key role in inflammation, tumorigenesis, development, and circulatory homeostasis. The PGD(2) metabolite 15-deoxy-Delta(12, 14) PGJ(2) (15d-PGJ(2)) was identified as a potent natural ligand for the peroxisome proliferator-activated receptor-gamma (PPARgamma). PPARgamma expressed in macrophages has been postulated as a negative regulator of inflammation and a positive regulator of differentiation into foam cell associated with atherogenesis. Here, we show that 15d-PGJ(2) suppresses the lipopolysaccharide (LPS)-induced expression of COX-2 in the macrophage-like differentiated U937 cells but not in vascular endothelial cells. PPARgamma mRNA abundantly expressed in the U937 cells, not in the endothelial cells, is down-regulated by LPS. In contrast, LPS up-regulates mRNA for the glucocorticoid receptor which ligand anti-inflammatory steroid dexamethasone (DEX) strongly suppresses the LPS-induced expression of COX-2, although both 15d-PGJ(2) and DEX suppressed COX-2 promoter activity by interfering with the NF-kappaB signaling pathway. Transfection of a PPARgamma expression vector into the endothelial cells acquires this suppressive regulation of COX-2 gene by 15d-PGJ(2) but not by DEX. A selective COX-2 inhibitor, NS-398, inhibits production of PGD(2) in the U937 cells. Taking these findings together, we propose that expression of COX-2 is regulated by a negative feedback loop mediated through PPARgamma, which makes possible a dynamic production of PG, especially in macrophages, and may be attributed to various expression patterns and physiological functions of COX-2.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta
  • Cattle
  • Cell Differentiation
  • Cells, Cultured
  • Cyclooxygenase 2
  • Dinoprostone / metabolism
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects
  • Endothelium, Vascular / physiology*
  • Feedback
  • Gene Expression Regulation, Enzymologic* / drug effects
  • Genes, Reporter
  • Humans
  • Isoenzymes / genetics*
  • Kinetics
  • Lipopolysaccharides / pharmacology*
  • Luciferases / genetics
  • Macrophages / drug effects
  • Macrophages / physiology*
  • Membrane Proteins
  • Prostaglandin D2 / analogs & derivatives*
  • Prostaglandin D2 / pharmacology
  • Prostaglandin-Endoperoxide Synthases / genetics*
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Recombinant Fusion Proteins / biosynthesis
  • Tetradecanoylphorbol Acetate / pharmacology
  • Transcription Factors / physiology*
  • Transcription, Genetic
  • Transfection
  • U937 Cells

Substances

  • 15-deoxy-delta(12,14)-prostaglandin J2
  • Isoenzymes
  • Lipopolysaccharides
  • Membrane Proteins
  • Receptors, Cytoplasmic and Nuclear
  • Recombinant Fusion Proteins
  • Transcription Factors
  • Luciferases
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Dinoprostone
  • Tetradecanoylphorbol Acetate
  • Prostaglandin D2