Salinomycin kills cancer stem cells by sequestering iron in lysosomes

Nat Chem. 2017 Oct;9(10):1025-1033. doi: 10.1038/nchem.2778. Epub 2017 May 16.

Abstract

Cancer stem cells (CSCs) represent a subset of cells within tumours that exhibit self-renewal properties and the capacity to seed tumours. CSCs are typically refractory to conventional treatments and have been associated to metastasis and relapse. Salinomycin operates as a selective agent against CSCs through mechanisms that remain elusive. Here, we provide evidence that a synthetic derivative of salinomycin, which we named ironomycin (AM5), exhibits a more potent and selective activity against breast CSCs in vitro and in vivo, by accumulating and sequestering iron in lysosomes. In response to the ensuing cytoplasmic depletion of iron, cells triggered the degradation of ferritin in lysosomes, leading to further iron loading in this organelle. Iron-mediated production of reactive oxygen species promoted lysosomal membrane permeabilization, activating a cell death pathway consistent with ferroptosis. These findings reveal the prevalence of iron homeostasis in breast CSCs, pointing towards iron and iron-mediated processes as potential targets against these cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Drug Screening Assays, Antitumor
  • Female
  • Homeostasis / drug effects
  • Humans
  • Iron / metabolism*
  • Lysosomes / chemistry
  • Lysosomes / drug effects*
  • Lysosomes / metabolism*
  • Molecular Conformation
  • Neoplastic Stem Cells / drug effects*
  • Neoplastic Stem Cells / metabolism
  • Neoplastic Stem Cells / pathology*
  • Pyrans / chemistry
  • Pyrans / pharmacology*
  • Reactive Oxygen Species / analysis
  • Reactive Oxygen Species / metabolism

Substances

  • Antineoplastic Agents
  • Pyrans
  • Reactive Oxygen Species
  • salinomycin
  • Iron