Metformin Exerts Antiproliferative and Anti-metastatic Effects Against Cholangiocarcinoma Cells by Targeting STAT3 and NF-ĸB

Anticancer Res. 2017 Jan;37(1):115-123. doi: 10.21873/anticanres.11296.

Abstract

Background/aim: Cholangiocarcinoma (CCA) is an aggressive cancer for which standard treatments are still ineffective. This study demonstrated the antiproliferative and anti-metastatic activity of metformin, an anti-diabetic drug, in CCA cells.

Materials and methods: Cell proliferation, migration/invasion and anoikis resistance were determined. The underlying mechanisms were identified using western blotting and immunocytofluorescence.

Results: Metformin significantly suppressed proliferation of CCA cells in a dose- and time-dependent manner, regardless of glucose present in the medium. A low dose of metformin significantly increased anoikis and inhibited migration/ invasion of CCA cells that was in concert with the decrease of vimentin, matrix metalloproteinase (MMP)-2 and -7. Activation of 5' adenosine monophosphate-activated protein kinase (AMPK) by phosphorylation together with suppression of nuclear translocation of signal transducer and activator of transcription 3 (STAT3) and nuclear factor-kappa B (NF-ĸB) were the underlying mechanisms for these effects.

Conclusion: Metformin is a potent antiproliferative and anti-metastatic agent against human CCA cells. These findings encourage the repurposing of metformin in clinical trials to improve CCA treatment.

Keywords: Metformin; NF-ĸB; STAT3; cholangiocarcinoma; proliferation.

MeSH terms

  • AMP-Activated Protein Kinases / metabolism
  • Anoikis / drug effects
  • Antineoplastic Agents / pharmacology*
  • Bile Duct Neoplasms / drug therapy*
  • Bile Duct Neoplasms / metabolism
  • Bile Duct Neoplasms / pathology
  • Cell Line, Tumor
  • Cell Movement / drug effects*
  • Cell Proliferation / drug effects*
  • Cholangiocarcinoma / drug therapy*
  • Cholangiocarcinoma / metabolism
  • Cholangiocarcinoma / pathology
  • Dose-Response Relationship, Drug
  • Humans
  • Metformin / pharmacology*
  • NF-kappa B / metabolism*
  • Neoplasm Invasiveness
  • Phosphorylation
  • STAT3 Transcription Factor / metabolism*
  • Signal Transduction / drug effects*
  • Time Factors

Substances

  • Antineoplastic Agents
  • NF-kappa B
  • STAT3 Transcription Factor
  • STAT3 protein, human
  • Metformin
  • AMP-Activated Protein Kinases