Regulation of cyclooxygenase-2 expression by iloprost in human vascular smooth muscle cells. Role of transcription factors CREB and ICER

Biochem Pharmacol. 2003 Mar 15;65(6):979-88. doi: 10.1016/s0006-2952(02)01661-1.

Abstract

Prostaglandin-endoperoxide synthase-2 (PGH-synthase) or cyclooxygenase-2 (COX-2) is inducible by a variety of stimuli, e.g. inflammatory mediators, growth factors and hormones and is believed to be responsible for the majority of inflammatory prostanoid production. Moreover, it has been demonstrated that COX-2 contributes substantially to prostacyclin-synthesis in patients with atherosclerosis. In this study, we demonstrate an up-regulation of COX-2 mRNA, protein and product formation by the prostacyclin-mimetic iloprost in human vascular smooth muscle cells (hSMC). COX-2 mRNA expression was induced transiently between 1 and 6 hr and returned to basal levels after 16 hr of iloprost stimulation. COX-2 protein was induced concomitantly between 3 and 6 hr of iloprost stimulation. This was accompanied by an increase in PGI(2) formation. Forskolin, a direct activator of adenylyl cyclase, and dibutyryl cAMP, a cell-permeable cAMP analogue-induced COX-2 mRNA, suggesting a cAMP-dependent COX-2 expression in hSMC. Iloprost-induced COX-2 protein expression and PGI(2) formation was synergistically elevated by co-stimulation with the phorbolester PMA (phorbol-12-myristate-13-acetate). It is concluded, that the observed up-regulation of COX-2 with subsequent release of newly synthesized PGI(2) and the synergistic effect of iloprost and phorbolester on PGI(2) formation provide a positive feedback of prostaglandins on their own synthesizing enzyme. This might be important for control of hSMC proliferation, migration and differentiation as well as inhibition of platelet aggregation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclic AMP / metabolism
  • Cyclic AMP Response Element Modulator
  • Cyclic AMP Response Element-Binding Protein / physiology*
  • Cyclooxygenase 2
  • DNA-Binding Proteins / physiology*
  • Epoprostenol / biosynthesis
  • Gene Expression / drug effects*
  • Humans
  • Iloprost / pharmacology*
  • Isoenzymes / biosynthesis*
  • Membrane Proteins
  • Muscle, Smooth, Vascular / drug effects*
  • Muscle, Smooth, Vascular / enzymology
  • Muscle, Smooth, Vascular / metabolism
  • Prostaglandin-Endoperoxide Synthases / biosynthesis*
  • RNA, Messenger / drug effects
  • RNA, Messenger / metabolism
  • Repressor Proteins*
  • Tetradecanoylphorbol Acetate / pharmacology
  • Time Factors
  • Vasodilator Agents / pharmacology

Substances

  • Cyclic AMP Response Element-Binding Protein
  • DNA-Binding Proteins
  • Isoenzymes
  • Membrane Proteins
  • RNA, Messenger
  • Repressor Proteins
  • Vasodilator Agents
  • Cyclic AMP Response Element Modulator
  • Epoprostenol
  • Cyclic AMP
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Iloprost
  • Tetradecanoylphorbol Acetate