Xanthohumol attenuates tumour cell-mediated breaching of the lymphendothelial barrier and prevents intravasation and metastasis

Arch Toxicol. 2013 Jul;87(7):1301-12. doi: 10.1007/s00204-013-1028-2. Epub 2013 Mar 17.

Abstract

Health beneficial effects of xanthohumol have been reported, and basic research provided evidence for anti-cancer effects. Furthermore, xanthohumol was shown to inhibit the migration of endothelial cells. Therefore, this study investigated the anti-metastatic potential of xanthohumol. MCF-7 breast cancer spheroids which are placed on lymphendothelial cells (LECs) induce "circular chemorepellent-induced defects" (CCIDs) in the LEC monolayer resembling gates for intravasating tumour bulks at an early step of lymph node colonisation. NF-κB reporter-, EROD-, SELE-, 12(S)-HETE- and adhesion assays were performed to investigate the anti-metastatic properties of xanthohumol. Western blot analyses were used to elucidate the mechanisms inhibiting CCID formation. Xanthohumol inhibited the activity of CYP, SELE and NF-kB and consequently, the formation of CCIDs at low micromolar concentrations. More specifically, xanthohumol affected ICAM-1 expression and adherence of MCF-7 cells to LECs, which is a prerequisite for CCID formation. Furthermore, markers of epithelial-to-mesenchymal transition (EMT) and of cell mobility such as paxillin, MCL2 and S100A4 were suppressed by xanthohumol. Xanthohumol attenuated tumour cell-mediated defects at the lymphendothelial barrier and inhibited EMT-like effects thereby providing a mechanistic explanation for the anti-intravasative/anti-metastatic properties of xanthohumol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid / metabolism
  • Antineoplastic Agents / pharmacology*
  • Biomarkers, Tumor / metabolism
  • Blotting, Western
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology*
  • Cell Adhesion / drug effects
  • Cell Movement / drug effects*
  • Coculture Techniques
  • Cytochrome P-450 CYP1A1 / metabolism
  • Dose-Response Relationship, Drug
  • E-Selectin / metabolism
  • Endothelial Cells / drug effects*
  • Endothelial Cells / metabolism
  • Endothelial Cells / pathology
  • Epithelial-Mesenchymal Transition / drug effects
  • Female
  • Flavonoids / pharmacology*
  • HEK293 Cells
  • Humans
  • Intercellular Adhesion Molecule-1 / metabolism
  • MCF-7 Cells
  • NF-kappa B / genetics
  • NF-kappa B / metabolism
  • Neoplasm Invasiveness
  • Propiophenones / pharmacology*
  • Spheroids, Cellular
  • Transfection

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • E-Selectin
  • Flavonoids
  • ICAM1 protein, human
  • NF-kappa B
  • Propiophenones
  • SELE protein, human
  • Intercellular Adhesion Molecule-1
  • 12-Hydroxy-5,8,10,14-eicosatetraenoic Acid
  • CYP1A1 protein, human
  • Cytochrome P-450 CYP1A1
  • xanthohumol