Sertaconazole, an Imidazole Antifungal Agent, Suppresses the Stemness of Breast Cancer Cells by Inhibiting Stat3 Signaling

In Vivo. 2025 Jan-Feb;39(1):190-200. doi: 10.21873/invivo.13817.

Abstract

Background/aim: Breast cancer stem cells (BCSCs) are a subpopulation of tumor cells that play a role in therapeutic resistance. In this study, we demonstrated that sertaconazole, an antifungal agent, displayed a potent inhibition on cancer stem cells (CSCs) and investigated the mechanism of action involved in its anti-BCSC effect.

Materials and methods: The effect of sertaconazole on BCSCs was investigated using a mammosphere formation assay, a colony formation assay, and a cell migration assay. In addition, CD44high/CD24low and ALDEFLOR analyses, an apoptosis assay, quantitative real-time PCR, western blotting, an electrophoretic mobility shift assay, and a cytokine profiling assay were performed.

Results: Sertaconazole inhibited cell proliferation, colony formation, cell migration, mammosphere formation, and mammosphere proliferation. It also induced apoptosis of breast cancer cells. It decreased the subpopulation of CD44high/CD24low and aldehyde dehydrogenase-expressing cells. It also reduced the DNA binding of Stat3 and nuclear protein expression levels of phosphorylated Stat3. Furthermore, it reduced the IL-8 mRNA levels of the mammosphere.

Conclusion: Sertaconazole can inhibit the Stat3 and IL-8 signaling pathways and induce CSC death. Thus, sertaconazole might be a potential inhibitor of BCSCs.

Keywords: Breast cancer stem cells; IL-8; Sertaconazole; Stat3.

MeSH terms

  • Antifungal Agents* / pharmacology
  • Apoptosis* / drug effects
  • Breast Neoplasms* / drug therapy
  • Breast Neoplasms* / genetics
  • Breast Neoplasms* / metabolism
  • Breast Neoplasms* / pathology
  • Cell Line, Tumor
  • Cell Movement* / drug effects
  • Cell Proliferation* / drug effects
  • Female
  • Humans
  • Imidazoles / pharmacology
  • Interleukin-8 / genetics
  • Interleukin-8 / metabolism
  • MCF-7 Cells
  • Neoplastic Stem Cells* / drug effects
  • Neoplastic Stem Cells* / metabolism
  • STAT3 Transcription Factor* / metabolism
  • Signal Transduction* / drug effects

Substances

  • STAT3 Transcription Factor
  • Antifungal Agents
  • STAT3 protein, human
  • Imidazoles
  • Interleukin-8