Silencing NOTCH signaling causes growth arrest in both breast cancer stem cells and breast cancer cells

Br J Cancer. 2013 Nov 12;109(10):2587-96. doi: 10.1038/bjc.2013.642. Epub 2013 Oct 15.

Abstract

Background: Breast cancer stem cells (BCSCs) are characterized by high aldehyde dehydrogenase (ALDH) enzyme activity and are refractory to current treatment modalities, show a higher risk for metastasis, and influence the epithelial to mesenchymal transition (EMT), leading to a shorter time to recurrence and death. In this study, we focused on examination of the mechanism of action of a small herbal molecule, psoralidin (Pso) that has been shown to effectively suppress the growth of BSCSs and breast cancer cells (BCCs), in breast cancer (BC) models.

Methods: ALDH(-) and ALDH(+) BCCs were isolated from MDA-MB-231 cells, and the anticancer effects of Pso were measured using cell viability, apoptosis, colony formation, invasion, migration, mammosphere formation, immunofluorescence, and western blot analysis.

Results: Psoralidin significantly downregulated NOTCH1 signaling, and this downregulation resulted in growth inhibition and induction of apoptosis in both ALDH(-) and ALDH(+) cells. Molecularly, Pso inhibited NOTCH1 signaling, which facilitated inhibition of EMT markers (β-catenin and vimentin) and upregulated E-cadherin expression, resulting in reduced migration and invasion of both ALDH(-) and ALDH(+) cells.

Conclusion: Together, our results suggest that inhibition of NOTCH1 by Pso resulted in growth arrest and inhibition of EMT in BCSCs and BCCs. Psoralidin appears to be a novel agent that targets both BCSCs and BCCs.

MeSH terms

  • Antineoplastic Agents, Phytogenic / pharmacology
  • Benzofurans / pharmacology
  • Breast Neoplasms / genetics
  • Breast Neoplasms / pathology*
  • Cell Movement / drug effects
  • Cell Movement / genetics
  • Cell Proliferation*
  • Coumarins / pharmacology
  • Drug Resistance, Neoplasm / drug effects
  • Drug Resistance, Neoplasm / genetics
  • Female
  • Gene Silencing*
  • Humans
  • Neoplasm Invasiveness
  • Neoplastic Stem Cells / drug effects
  • Neoplastic Stem Cells / metabolism
  • Neoplastic Stem Cells / pathology*
  • Receptor, Notch1 / antagonists & inhibitors
  • Receptor, Notch1 / genetics*
  • Signal Transduction / drug effects
  • Signal Transduction / genetics
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents, Phytogenic
  • Benzofurans
  • Coumarins
  • NOTCH1 protein, human
  • Receptor, Notch1
  • psoralidin