Cyclooxygenase-2 expression by nonsteroidal anti-inflammatory drugs in human airway smooth muscle cells: role of peroxisome proliferator-activated receptors

J Immunol. 2003 Jan 15;170(2):1043-51. doi: 10.4049/jimmunol.170.2.1043.

Abstract

Nonsteroidal anti-inflammatory drugs (NSAIDs) have been shown to modulate cyclooxygenase (COX)-2 expression, but the mechanisms involved are controversial and may be cell specific. We show in this study that indomethacin (Indo), flurbiprofen (Flur), and the selective COX-2 inhibitor NS-398 induced COX-2 expression and markedly enhanced IL-1beta-induced COX-2 expression in human airway smooth muscle (HASM) cells. These effects were not reversed by exogenous PGE(2), suggesting that they are prostanoid-independent. Indeed, PGE(2) also induced and enhanced IL-1beta-induced COX-2 expression. Peroxisome proliferator-activated receptor (PPAR) alpha and PPARgamma (not PPARbeta) were expressed in HASM cells. PPARgamma activators ciglitizone (Cig) and 15-Deoxy-Delta(12,14)-PGJ(2) (15d-PGJ(2)), but not the PPARalpha activator WY-14643, mimicked the effect of NSAIDs on COX-2 expression. Treatment with Flur, NS-398, Cig, and 15d-PGJ(2) alone, but not Indo and WY-14643, elevated COX activity; however, neither enhanced IL-1beta-induced COX activity. Pretreatment with dexamethasone suppressed COX-2 expression, PGE(2) release, and COX activity induced by NS-398, Cig, IL-1beta, alone or in combination. Unlike IL-1beta, NS-398 and Cig did not cause NF-kappaB (p65) nuclear translocation, nor did they further enhance IL-1beta-induced NF-kappaB translocation, but they stimulated PPARgamma translocation. Indo, NS-398, Flur, and 15d-PGJ(2), but not WY-14643, induced transcriptional activity of a COX-2 reporter construct containing the peroxisome proliferator response element (PPRE) on their own and enhanced the effect of IL-1beta, but had no effect on a COX-2 reporter construct lacking the PPRE. The results suggest that COX-2 expression by NSAIDs is biologically functional, prostanoid-independent, and involves PPARgamma activation, and provide the first direct evidence that the PPRE in the promoter is required for NSAID-induced COX-2 expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / pharmacology
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Cell Survival / genetics
  • Cyclooxygenase 2
  • Dexamethasone / pharmacology
  • Dinoprostone / biosynthesis
  • Dinoprostone / metabolism
  • Flurbiprofen / pharmacology
  • Humans
  • Indomethacin / pharmacology
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / biosynthesis*
  • Isoenzymes / genetics
  • Isoenzymes / metabolism
  • Lung / cytology
  • Lung / drug effects
  • Lung / enzymology*
  • Lung / metabolism
  • Membrane Proteins
  • Muscle, Smooth / cytology
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / enzymology*
  • Muscle, Smooth / metabolism
  • NF-kappa B / metabolism
  • Nitrobenzenes / pharmacology
  • Promoter Regions, Genetic / drug effects
  • Prostaglandin Antagonists / pharmacology
  • Prostaglandin D2 / analogs & derivatives
  • Prostaglandin D2 / pharmacology
  • Prostaglandin-Endoperoxide Synthases / biosynthesis*
  • Prostaglandin-Endoperoxide Synthases / genetics
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Prostaglandins / physiology
  • Protein Transport / drug effects
  • Receptors, Cytoplasmic and Nuclear / biosynthesis
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Response Elements / genetics
  • Sulfonamides / pharmacology
  • Thiazoles / pharmacology
  • Thiazolidinediones*
  • Transcription Factors / biosynthesis
  • Transcription Factors / genetics
  • Transcription Factors / metabolism
  • Transcription Factors / physiology*
  • Transcriptional Activation / drug effects

Substances

  • 15-deoxy-delta(12,14)-prostaglandin J2
  • Adjuvants, Immunologic
  • Anti-Inflammatory Agents, Non-Steroidal
  • Isoenzymes
  • Membrane Proteins
  • NF-kappa B
  • Nitrobenzenes
  • Prostaglandin Antagonists
  • Prostaglandins
  • Receptors, Cytoplasmic and Nuclear
  • Sulfonamides
  • Thiazoles
  • Thiazolidinediones
  • Transcription Factors
  • N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide
  • Flurbiprofen
  • Dexamethasone
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Dinoprostone
  • Prostaglandin D2
  • ciglitazone
  • Indomethacin