Rosuvastatin reduces interleukin-6-induced expression of C-reactive protein in human hepatocytes in a STAT3- and C/EBP-dependent fashion

Int J Clin Pharmacol Ther. 2007 Jun;45(6):319-27. doi: 10.5414/cpp45319.

Abstract

Objective: It has been speculated that the reduction in vascular events by statins may not only be due to lowering of cholesterol, but also to the decrease in plasma C-reactive protein (CRP). In the present study we investigated the possibility that rosuvastatin directly affected CRP expression in stimulated human hepatocytes.

Methods: Interleukin 6 (IL-6) stimulated human hepatoma cells (Hep3B) and primary human hepatocytes (PHH) were incubated with various concentrations of rosuvastatin (0.3 - 1 microM) for 24 hours. CRP expression was determined using ELISA and quantitative real-time RT-PCR. The activation of STAT3 and C/EBP was investigated utilizing transcription factor assays (TransAM).

Results: IL-6 increased CRP secretion by up to 5-fold in Hep3B and 6.6-fold in PHH. Rosuvastatin reduced CRP expression by 32% and 46% in Hep3B and PHH, respectively. IL-6 increased CRP mRNA up to 32-fold. At 1 microM, rosuvastatin reduced CRP mRNA by 73% compared to IL-6-stimulated cells. IL-6 activated the transcription factors STAT3 and C/EBP up to 2.6-fold and 2.2-fold, respectively. Rosuvastatin (1 microM) attenuated the activation of STAT3 and C/EBP by 48% and 54%, respectively.

Conclusions: Our results show a direct inhibitory effect of rosuvastatin on IL-6-induced expression of CRP in liver cells. Statins may lower CRP by inhibiting its production in the liver rather than by exerting systemic anti-inflammatory effects. The effects of rosuvastatin in reducing the levels of CRP in plasma may have clinical utility in addition to its effects on atherogenic lipoproteins.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Atorvastatin
  • C-Reactive Protein / biosynthesis*
  • CCAAT-Enhancer-Binding Proteins / physiology*
  • Cells, Cultured
  • Fluorobenzenes / pharmacology*
  • Hepatocytes / drug effects
  • Hepatocytes / metabolism*
  • Heptanoic Acids / pharmacology
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacology*
  • Immunoassay
  • Interleukin-6 / antagonists & inhibitors*
  • Interleukin-6 / pharmacology*
  • Mevalonic Acid / pharmacology
  • Pyrimidines / pharmacology*
  • Pyrroles / pharmacology
  • RNA, Messenger / biosynthesis
  • RNA, Messenger / genetics
  • Rosuvastatin Calcium
  • STAT3 Transcription Factor / physiology*
  • Sulfonamides / pharmacology*
  • Transcription Factors

Substances

  • CCAAT-Enhancer-Binding Proteins
  • Fluorobenzenes
  • Heptanoic Acids
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Interleukin-6
  • Pyrimidines
  • Pyrroles
  • RNA, Messenger
  • STAT3 Transcription Factor
  • Sulfonamides
  • Transcription Factors
  • Rosuvastatin Calcium
  • C-Reactive Protein
  • Atorvastatin
  • Mevalonic Acid