Pravastatin down-regulates inflammatory mediators in human monocytes in vitro

Eur J Pharmacol. 2000 Dec 20;410(1):83-92. doi: 10.1016/s0014-2999(00)00870-0.

Abstract

There is experimental evidence that pravastatin, which is designed to inhibit the rate-limiting enzyme of cholesterol synthesis, can affect cell metabolism and proliferation. We therefore studied the effects of pravastatin on the generation of inflammatory mediators in non-stimulated and stimulated primary human monocytes in vitro. In our experimental model, pravastatin induced a dose-dependent inhibition of monocyte cholesterol synthesis (up to 67%), up-regulation of low density lipoprotein receptor mRNA (by about 35%) and reduction in intracellular cholesterol accumulation. In parallel, exposure of non-stimulated monocytes to various doses of pravastatin resulted in inhibition of monocyte chemoattractant protein-1 protein expression (up to 15-fold), reduction of tumour necrosis factor alpha (TNF-alpha) levels (up to 2.4-fold) and a total loss of metalloproteinase-9 activity in stimulated cells. Pravastatin at concentrations of 5, 100 and 500 microM caused an inhibition of TNF-alpha-induced cellular oxygen consumption from 2. 4- to 5.5-fold. These data extend the findings of potential anti-inflammatory actions of statins and also suggest the possibility for pravastatin use in a broader spectrum of inflammatory situations.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemokine CCL2 / metabolism
  • Cholesterol / biosynthesis
  • DNA Primers / chemistry
  • Dose-Response Relationship, Drug
  • Down-Regulation
  • Enzyme-Linked Immunosorbent Assay
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology*
  • In Vitro Techniques
  • Inflammation Mediators / metabolism*
  • Interleukin-6 / metabolism
  • Lipoproteins, LDL / metabolism
  • Metalloendopeptidases / metabolism
  • Monocytes / drug effects*
  • Monocytes / metabolism
  • Oxygen Consumption / drug effects
  • Pravastatin / pharmacology*
  • RNA, Messenger / metabolism
  • Receptors, LDL / genetics
  • Reverse Transcriptase Polymerase Chain Reaction
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Chemokine CCL2
  • DNA Primers
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Inflammation Mediators
  • Interleukin-6
  • Lipoproteins, LDL
  • RNA, Messenger
  • Receptors, LDL
  • Tumor Necrosis Factor-alpha
  • Cholesterol
  • Metalloendopeptidases
  • Pravastatin