1,2,3,4,6-Penta-O-galloyl-beta-D-glucose blocks endothelial cell growth and tube formation through inhibition of VEGF binding to VEGF receptor

Cancer Lett. 2004 May 10;208(1):89-94. doi: 10.1016/j.canlet.2003.11.008.


Tumor angiogenesis is a critical step for the growth and metastasis of solid tumors. Vascular endothelial growth factor (VEGF) is the most important angiogenic molecule associated with tumor-induced neovascularization. VEGF exerts its activity through binding to its receptor tyrosine kinase, KDR/Flk-1, expressed on the surface of endothelial cells. From the screening of medicinal plants, we have identified 1,2,3,4,6-penta-O-galloyl-beta-d-glucose (PGG) from the roots of Paeonia lactiflora that inhibited the binding of VEGF to KDR/Flk-1. PGG efficiently blocked VEGF-induced human umbilical vein endothelial cell proliferation and the growth of immortalized human microvascular endothelial cells, but did not affect the growth of HT1080 human fibrosarcoma and DU-145 human prostate carcinoma cells. PGG also blocked VEGF-induced capillary-like tube formation of endothelial cell on Matrigel. Our results suggest that PGG could be a candidate for developing anti-angiogenic agent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Division / drug effects
  • Cell Movement
  • Collagen / chemistry
  • Drug Combinations
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects*
  • Fibrosarcoma / metabolism
  • Fibrosarcoma / pathology
  • Humans
  • Hydrolyzable Tannins*
  • Laminin / chemistry
  • Male
  • Paeonia / chemistry
  • Plant Extracts / chemistry
  • Prostatic Neoplasms / pathology
  • Protein Binding / drug effects*
  • Proteoglycans / chemistry
  • Receptors, Vascular Endothelial Growth Factor / metabolism*
  • Sodium-Potassium-Exchanging ATPase / antagonists & inhibitors
  • Tannins / pharmacology*
  • Umbilical Veins / metabolism
  • Vascular Endothelial Growth Factor A / metabolism*


  • Drug Combinations
  • Hydrolyzable Tannins
  • Laminin
  • Plant Extracts
  • Proteoglycans
  • Tannins
  • Vascular Endothelial Growth Factor A
  • matrigel
  • beta-penta-O-galloyl-glucose
  • Collagen
  • Receptors, Vascular Endothelial Growth Factor
  • Sodium-Potassium-Exchanging ATPase