Synergistic killing of glioblastoma stem-like cells by bortezomib and HDAC inhibitors

Anticancer Res. 2012 Jul;32(7):2407-13.

Abstract

Background: The malignant brain tumour glioblastoma is a devastating disease that remains a therapeutic challenge.

Materials and methods: Effects of combinations of the US Food and Drug Administation (FDA) approved proteasome inhibitor bortezomib and the histone deacetylase (HDAC) inhibitors vorinostat, valproic acid and sodium phenylbutyrate were studied on primary glioblastoma stem cell lines and conventional glioblastoma cell lines. Cell survival, proliferation and death were analyzed by fluorometric microculture cytotoxicity assay (FMCA), propidium iodide labeling and flow cytometry, and cell cloning through limiting dilution and live-cell bright-field microscopy.

Results: Bortezomib and the HDAC inhibitors showed synergistic cell killing at clinically relevant drug concentrations, while the conventional cell lines cultured in serum-containing medium were relatively resistant to the same treatments.

Conclusion: These findings of synergistic glioblastoma stem cell killing by bortezomib and three different FDA-approved HDAC inhibitors confirm and expand previous observations on co-operative effects between these classes of drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Apoptosis / drug effects
  • Boronic Acids / administration & dosage
  • Boronic Acids / pharmacology*
  • Bortezomib
  • Brain Neoplasms / drug therapy*
  • Brain Neoplasms / pathology
  • Cell Line, Tumor
  • Drug Synergism
  • Glioblastoma / drug therapy*
  • Glioblastoma / pathology
  • Histone Deacetylase Inhibitors / administration & dosage
  • Histone Deacetylase Inhibitors / pharmacology*
  • Humans
  • Hydroxamic Acids / administration & dosage
  • Hydroxamic Acids / pharmacology
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / pathology
  • Neural Stem Cells / drug effects*
  • Neural Stem Cells / pathology
  • Phenylbutyrates / administration & dosage
  • Phenylbutyrates / pharmacology
  • Pyrazines / administration & dosage
  • Pyrazines / pharmacology*
  • Valproic Acid / administration & dosage
  • Valproic Acid / pharmacology
  • Vorinostat

Substances

  • Boronic Acids
  • Histone Deacetylase Inhibitors
  • Hydroxamic Acids
  • Phenylbutyrates
  • Pyrazines
  • Vorinostat
  • Valproic Acid
  • Bortezomib