Esculin and its oligomer fractions inhibit adhesion and migration of U87 glioblastoma cells and in vitro angiogenesis

Tumour Biol. 2016 Mar;37(3):3657-64. doi: 10.1007/s13277-015-4209-1. Epub 2015 Oct 12.

Abstract

Cancer metastasis is the major cause of cancer-related death. Chemoprevention is defined as the use of natural or synthetic substances to prevent cancer formation or cancer progress. In the present study, we investigate the antitumor activity of esculin and its oligomer fractions in U87 glioblastoma cells. We showed that esculin and its oligomers reduced U87 cell growth in a dose dependent manner. They also inhibited cell adhesion to collagen IV and vitronectin by interfering with the function of their respective receptors α2β1 and αvβ5 integrins. Furthermore, the tested samples were able to reduce migration of U87 cells towards another extracellular matrix fibronectin. Moreover, esculin and its oligomer fractions inhibited in vitro angiogenesis of endothelial cells (HMEC-1). In summary, our data provide the first evidence that esculin and its oligomer fractions are able to reduce adhesion, migration of glioblastoma cells and in vitro angiogenesis. Esculin and its oligomers may thus exert multi-target functions against cancer cells.

Keywords: Angiogenesis; Esculin; Glioblastoma; Migration; Oligomer fractions.

MeSH terms

  • Cell Adhesion / drug effects
  • Cell Line, Tumor
  • Cell Movement / drug effects*
  • Cell Proliferation / drug effects*
  • Cell Survival / drug effects
  • Dimerization
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Esculin / chemistry
  • Esculin / pharmacology*
  • Glioblastoma / blood supply
  • Glioblastoma / metabolism
  • Glioblastoma / pathology
  • Humans
  • Integrin alpha2beta1 / metabolism
  • Neovascularization, Pathologic / metabolism
  • Neovascularization, Pathologic / prevention & control
  • Receptors, Vitronectin / metabolism

Substances

  • Integrin alpha2beta1
  • Receptors, Vitronectin
  • integrin alphaVbeta5
  • Esculin