Bavachin Induces Ferroptosis through the STAT3/P53/SLC7A11 Axis in Osteosarcoma Cells

Oxid Med Cell Longev. 2021 Oct 18:2021:1783485. doi: 10.1155/2021/1783485. eCollection 2021.

Abstract

Ferroptosis is a new form of regulated cell death, which is mediated by intracellular iron. Although it is reported that bavachin has antitumour effects on several tumour cells and prompts the reactive oxygen species (ROS) generation, it is unclear whether ferroptosis can be induced by bavachin in osteosarcoma (OS) cells. In this study, we found that bavachin inhibits the viability of MG63 and HOS OS cell lines along with an increase in the ferrous iron level, ROS accumulation, malondialdehyde overexpression, and glutathione depletion. Moreover, iron chelators (deferoxamine), antioxidants (Vit E), and ferroptosis inhibitors (ferrostatin-1 and liproxstatin-1) reverse bavachin-induced cell death. Bavachin also altered the mitochondrial morphology of OS cells, leading to smaller mitochondria, higher density of the mitochondrial membrane, and reduced mitochondrial cristae. Further investigation showed that bavachin upregulated the expression of transferrin receptor, divalent metal transporter-1, and P53, along with downregulating the expression of ferritin light chain, ferritin heavy chain, p-STAT3 (705), SLC7A11, and glutathione peroxidase-4 in OS cells. More importantly, STAT3 overexpression, SLC7A11 overexpression, and pretreatment with pifithrin-α (P53 inhibitor) rescued OS cell ferroptosis induced by bavachin. The results show that bavachin induces ferroptosis via the STAT3/P53/SLC7A11 axis in OS cells.

MeSH terms

  • Amino Acid Transport System y+ / genetics
  • Amino Acid Transport System y+ / metabolism*
  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Bone Neoplasms / drug therapy*
  • Bone Neoplasms / genetics
  • Bone Neoplasms / metabolism
  • Bone Neoplasms / ultrastructure
  • Cell Line, Tumor
  • Ferroptosis / drug effects*
  • Flavonoids / pharmacology*
  • Humans
  • Iron / metabolism
  • Mitochondria / drug effects
  • Mitochondria / metabolism
  • Mitochondria / ultrastructure
  • Osteosarcoma / drug therapy*
  • Osteosarcoma / genetics
  • Osteosarcoma / metabolism
  • Osteosarcoma / ultrastructure
  • Phospholipid Hydroperoxide Glutathione Peroxidase / metabolism
  • Phosphorylation
  • Reactive Oxygen Species / metabolism
  • STAT3 Transcription Factor / genetics
  • STAT3 Transcription Factor / metabolism*
  • Signal Transduction
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • Amino Acid Transport System y+
  • Antineoplastic Agents, Phytogenic
  • Flavonoids
  • Reactive Oxygen Species
  • SLC7A11 protein, human
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • TP53 protein, human
  • Tumor Suppressor Protein p53
  • bavachin
  • Iron
  • Phospholipid Hydroperoxide Glutathione Peroxidase