C-jun N-terminal kinase (JNK) inhibitor, SP600125, blocks interleukin (IL)-6-induced vascular endothelial growth factor (VEGF) production: cyclosporine A partially mimics this inhibitory effect

Transplantation. 2003 Nov 15;76(9):1380-2. doi: 10.1097/01.TP.0000085661.52980.95.

Abstract

Angiogenesis is a common complication of organ-transplant rejection. One of the primary responsible molecules for enhanced angiogenesis is vascular endothelial growth factor (VEGF). Activated protein (AP)-1 is considered to play a key role in the transcription of VEGF. c-jun N-terminal kinase (JNK), one of the MAP kinase family members, plays a critical role in AP-1 activation. Thus, we tested the effect of a novel JNK inhibitor, SP600125, on VEGF production in fibroblasts. SP600125 significantly suppressed interleukin (IL)-6-induced production of VEGF in cultured fibroblasts. Cyclosporine A (CsA), a known in vitro anti-angiogenic reagent, partially mimicked this suppression. In fact, CsA suppressed IL-6-induced phosphorylation of JNK. The results indicate that although both SP600125 and CsA are anti-angiogenic by inhibiting VEGF production by way of a JNK-dependent pathway, the inhibitory effect was much stronger with the novel inhibitor of JNK than with CsA.

Publication types

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

MeSH terms

  • Anthracenes / pharmacology*
  • Cells, Cultured
  • Cyclosporine / pharmacology*
  • Enzyme Inhibitors / pharmacology*
  • Fibroblasts / cytology
  • Fibroblasts / immunology
  • Gingiva / drug effects
  • Gingiva / immunology
  • Gingiva / physiology
  • Humans
  • Interleukin-6 / antagonists & inhibitors*
  • JNK Mitogen-Activated Protein Kinases
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • Neovascularization, Pathologic / prevention & control
  • Phosphorylation
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / genetics*

Substances

  • Anthracenes
  • Enzyme Inhibitors
  • Interleukin-6
  • Vascular Endothelial Growth Factor A
  • pyrazolanthrone
  • Cyclosporine
  • JNK Mitogen-Activated Protein Kinases
  • Mitogen-Activated Protein Kinases