FGF-2-mediated FGFR1 signaling in human microvascular endothelial cells is activated by vaccarin to promote angiogenesis

Biomed Pharmacother. 2017 Nov:95:144-152. doi: 10.1016/j.biopha.2017.08.059. Epub 2017 Sep 12.

Abstract

Angiogenesis is a complex physiological process involving the growth of new capillaries. The impaired angiogenesis plays important roles in chronic wounds and ischaemic heart disease. Fibroblast growth factor 2 (FGF-2) exerts pro-angiogenic actions via activation of fibroblast growth factor receptor 1 (FGFR-1). We have identified that vaccarin increased the angiogenic activity of endothelial cells. In this study, we investigated whether FGF-2-mediated FGFR1 signaling pathway participated in vaccarin-mediated neovascularization formation. Human microvascular endothelial cells (HMEC)-1 were incubated with various doses of vaccarin. Our results showed that vaccarin dose-dependently up-regulated FGF-2 levels and phosphorylation of FGFR-1. Neutralization of FGF-2 with anti-FGF-2 antibody also abolished the proliferation, migration and tube formation of HMEC-1 cells induced by vaccarin. Both FGFR-1 inhibitor SU5402 and FGFR-1 siRNA blocked vaccarin-induced cell cycle progression and angiogenesis. The mouse Matrigel model study further unveiled that vaccarin stimulated the neovascularization and microvessel density in vivo, which was prevented by FGFR-1 inhibitor SU5402. Taken together, our results demonstrated for the first time that vaccarin was a novel inducer for FGF-2 expression, followed by phosphorylation of FGFR-1 and subsequent angiogenic behaviors in endothelial cells. Vaccarin may be a promising candidate of angiogenesis activator for neurovascular repair or therapy.

Keywords: Angiogenesis; Endothelial cells; Fibroblast growth gactor-2; Migration; Proliferation.

MeSH terms

  • Animals
  • Cell Cycle
  • Cell Line
  • Cell Movement
  • Cell Proliferation
  • Collagen
  • Drug Combinations
  • Endothelial Cells / physiology*
  • Fibroblast Growth Factor 2 / genetics
  • Fibroblast Growth Factor 2 / metabolism*
  • Flavonoids / chemistry
  • Flavonoids / metabolism*
  • Gene Expression Regulation / drug effects*
  • Glycosides / administration & dosage
  • Glycosides / chemistry
  • Glycosides / metabolism
  • Glycosides / pharmacology*
  • Humans
  • Laminin
  • Mice
  • Mice, Inbred ICR
  • Neovascularization, Physiologic
  • Proteoglycans
  • RNA Interference
  • Receptor, Fibroblast Growth Factor, Type 1 / genetics
  • Receptor, Fibroblast Growth Factor, Type 1 / metabolism*
  • Signal Transduction

Substances

  • Drug Combinations
  • Flavonoids
  • Glycosides
  • Laminin
  • Proteoglycans
  • vaccarin H
  • Fibroblast Growth Factor 2
  • matrigel
  • Collagen
  • FGFR1 protein, human
  • Fgfr1 protein, mouse
  • Receptor, Fibroblast Growth Factor, Type 1