Potent angiogenic inhibition effects of deacetylated chitohexaose separated from chitooligosaccharides and its mechanism of action in vitro

Carbohydr Res. 2009 Oct 12;344(15):1975-83. doi: 10.1016/j.carres.2009.06.036. Epub 2009 Jul 23.

Abstract

This study was performed to demonstrate the effects of deacetylated chitohexaose (hexamer) separated from a chitooligosaccharide (COS) mixture on tumor angiogenesis and its mechanism of action. Five fractions from dimer to hexamer were separated by a linear gradient solution of HCl on a cation-exchange resin. Then HCl was removed from the fractions by a charcoal column. The purity of the five fractions was analyzed by HPLC and the molecular masses were analyzed by MALDI-TOFMS. The hexamer expressed an inhibitory influence on CAM angiogenesis in a dose-dependent manner at concentrations of 6.25-50microg/egg. On further investigation, we found that the hexamer had no toxic effect on normal ECV304 cells, but could inhibit the proliferation and migration of tumor-induced ECV304 cells in a dose-dependent manner. The mechanism was demonstrated through the detection of mRNA expression of VEGF, MMP-9, TIMP-1, TIMP-2, and uPA by RT-PCR, which showed that the hexamer down-regulated the VEGF and uPA mRNA expressions in ECV304 cells, but up-regulated the TIMP-1 mRNA expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Chitosan / chemistry*
  • Chromatography, High Pressure Liquid
  • Gene Expression / drug effects
  • Humans
  • Matrix Metalloproteinase 9 / genetics
  • Molecular Structure
  • Neovascularization, Physiologic / drug effects*
  • Oligosaccharides / chemistry*
  • Oligosaccharides / pharmacology*
  • Reverse Transcriptase Polymerase Chain Reaction
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
  • Tissue Inhibitor of Metalloproteinase-1 / genetics
  • Tissue Inhibitor of Metalloproteinase-2 / genetics
  • Urokinase-Type Plasminogen Activator / genetics
  • Vascular Endothelial Growth Factor A / genetics

Substances

  • Oligosaccharides
  • Tissue Inhibitor of Metalloproteinase-1
  • Vascular Endothelial Growth Factor A
  • Tissue Inhibitor of Metalloproteinase-2
  • chitohexaose
  • Chitosan
  • Urokinase-Type Plasminogen Activator
  • Matrix Metalloproteinase 9