Protective effects of ligustrazine on TNF-α-induced endothelial dysfunction

Eur J Pharmacol. 2012 Jan 15;674(2-3):365-9. doi: 10.1016/j.ejphar.2011.10.046. Epub 2011 Nov 7.

Abstract

To investigate the effects of Ligustrazine, a compound derived from chuanxiong, on tumor necrosis factor-α (TNF-α) stimulated endothelial cells. Human umbilical vein endothelial cells (HUVECs) were stimulated with TNF-α in vitro. Nitric oxide (NO) was measured as a standard of endothelial dysfunction. Two important indicators of autoimmunity, intracellular adhesion molecular-1 (ICAM-1) and heat shock protein 60 (HSP60), were selected to evaluate the influence of Ligustrazine on HUVECs. Ligustrazine (40 μg/ml) significantly reversed the decrease in NO production induced by TNF-α (5 ng/ml) in HUVECs. The expressions of ICAM-1 and HSP60 were increased by TNF-α treatment, but dramatically inhibited by treatment with ligustrazine in TNF-α-stimulated cells. Ligustrazine increased the production of NO in HUVECs and had an immunomodulatory effect on HUVECs stimulated with TNF-α by down-regulating the expression of ICAM-1 and HSP60. These results suggest that ligustrazine protects the endothelium via inhibition of immunological reactions, preventing atherosclerosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Autoimmunity / drug effects
  • Biomarkers / metabolism
  • Chaperonin 60 / metabolism
  • Down-Regulation / drug effects
  • Human Umbilical Vein Endothelial Cells / drug effects*
  • Human Umbilical Vein Endothelial Cells / immunology
  • Human Umbilical Vein Endothelial Cells / metabolism
  • Human Umbilical Vein Endothelial Cells / pathology
  • Humans
  • Inflammation / immunology
  • Inflammation / metabolism
  • Inflammation / pathology
  • Intercellular Adhesion Molecule-1 / metabolism
  • Nitric Oxide / biosynthesis
  • Pyrazines / pharmacology*
  • Tumor Necrosis Factor-alpha / pharmacology*

Substances

  • Biomarkers
  • Chaperonin 60
  • Pyrazines
  • Tumor Necrosis Factor-alpha
  • Intercellular Adhesion Molecule-1
  • Nitric Oxide
  • tetramethylpyrazine