Oxidized phospholipids inhibit cyclooxygenase-2 in human macrophages via nuclear factor-kappaB/IkappaB- and ERK2-dependent mechanisms

Cardiovasc Res. 2002 Aug 1;55(2):406-15. doi: 10.1016/s0008-6363(02)00437-6.

Abstract

Objective: Oxidized low-density lipoproteins (ox-LDL) or their components suppress macrophage inflammatory response by down-regulating cytokine synthesis, nitric oxide synthase and inducible cyclooxygenase (Cox-2). This event is crucial for the pathophysiological process leading to the formation of atherosclerotic plaque. Our present study focused on the mechanisms through which oxidized phospholipids inhibit LPS-induced Cox-2 expression in human macrophages.

Methods: Macrophages were incubated with a mixture of oxidized fragmented phospholipids (ox-PAPC), present in modified LDL, and then exposed to LPS. Cox-2 was evaluated in terms of protein levels, mRNA and activity.

Results: Ox-PAPC dose-dependently inhibited Cox-2 protein, mRNA and activity by preventing NF-kappaB binding to DNA. This effect was consequent to alterations of the degradation pattern of IkappaBalpha. Moreover, ox-PAPC markedly prevented extracellular signal-regulated kinase (ERK2) activation, leading to Cox-2 expression, whereas activation of the transcription factor peroxisome proliferator-activated receptors (PPARs) was not influenced.

Conclusion: ox-PAPC down-regulates LPS-induced Cox-2 expression in human macrophages by targeting both NF-kappaB/IkappaB and ERK2 pathways. An altered inflammatory response by macrophages within atheromata may contribute to the progression of atherosclerosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Culture Techniques
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Down-Regulation / drug effects
  • Humans
  • I-kappa B Proteins / physiology
  • Isoenzymes / antagonists & inhibitors*
  • Isoenzymes / genetics
  • Lipopolysaccharides / pharmacology
  • Lipoproteins, LDL / pharmacology*
  • Macrophages / drug effects*
  • Macrophages / enzymology
  • Membrane Proteins
  • Mitogen-Activated Protein Kinases / physiology
  • NF-kappa B / physiology*
  • Prostaglandin-Endoperoxide Synthases / genetics
  • RNA, Messenger / genetics

Substances

  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • I-kappa B Proteins
  • Isoenzymes
  • Lipopolysaccharides
  • Lipoproteins, LDL
  • Membrane Proteins
  • NF-kappa B
  • RNA, Messenger
  • oxidized low density lipoprotein
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Mitogen-Activated Protein Kinases