Xanthohumol Sensitizes Melanoma Cells to Vemurafenib by Lowering Membrane Cholesterol and Increasing Membrane Fluidity

Int J Mol Sci. 2025 Mar 4;26(5):2290. doi: 10.3390/ijms26052290.

Abstract

Chemoresistance remains one of the major obstacles to cancer treatment. The search for specific molecules that could improve cancer treatment has become one of the objectives of biomedical research. Identifying new natural molecules to enhance chemotherapy treatment or improve sensitization to conventional therapies has become a key objective. Here, we evaluated the effect of Xanthohumol (XN) extracted from hop on SKMEL-28 melanoma cells and their sensitization to vemurafenib (VEM) treatment. We measured the XN effect on cell viability and apoptosis. We also assessed the effect of XN on membrane fluidity and membrane cholesterol levels. Finally, we studied the impact of XN on cell sensitization to VEM. Here, we showed that XN reduced SKMEL-28 cell viability through an apoptotic mechanism. Our results demonstrated the potential role of XN in sensitizing cancer cells to VEM with a less toxic effect on non-tumor cells. A study of XN's molecular mechanism showed that XN was able to induce cholesterol depletion and increased fluidity in SKMEL-28 cancer cells. This leads to an increase in VEM incorporation. Here, we describe the importance of the strategy to modulate membrane fluidity by XN in order to significantly improve anticancer therapy.

Keywords: chemoresistance; melanoma cancer; membrane fluidity; natural compound; vemurafenib; xanthohumol.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Apoptosis* / drug effects
  • Cell Line, Tumor
  • Cell Membrane* / drug effects
  • Cell Membrane* / metabolism
  • Cell Survival / drug effects
  • Cholesterol* / metabolism
  • Drug Synergism
  • Flavonoids* / pharmacology
  • Humans
  • Melanoma* / drug therapy
  • Melanoma* / metabolism
  • Melanoma* / pathology
  • Membrane Fluidity* / drug effects
  • Propiophenones* / pharmacology
  • Vemurafenib* / pharmacology

Substances

  • Propiophenones
  • xanthohumol
  • Cholesterol
  • Vemurafenib
  • Flavonoids
  • Antineoplastic Agents

Grants and funding

This work was supported by the University of Reims Champagne Ardennes, the Center National de la Recherche Scientifique (CNRS) and Fonds régional de coopération pour la recherche de la région Grand-Est, France.