SIRT1 contributes in part to cisplatin resistance in cancer cells by altering mitochondrial metabolism

Mol Cancer Res. 2008 Sep;6(9):1499-506. doi: 10.1158/1541-7786.MCR-07-2130. Epub 2008 Aug 22.

Abstract

Tumors frequently develop resistance to cisplatin, a platinum drug used as a cornerstone of present-day chemotherapy regimens, significantly decreasing its usefulness in the clinic. Although it is known that cisplatin-resistant (CP-r) cancer cells commonly grow more slowly and exhibit reduced uptake of various compounds, including nutrients, the effect of tumor metabolism on cisplatin resistance is unclear. It was found that in CP-r cells, uptake of 2-deoxyglucose was reduced due to dysfunction and altered morphology of mitochondria compared with cisplatin-sensitive parental cancer cells. The CP-r cells overexpressed SIRT1, a histone deacetylase that plays a central role in DNA damage response and transcriptional silencing. Incubation of drug-sensitive cells in low glucose medium induced the expression of SIRT1 and increased cellular resistance to cisplatin. Reduced SIRT1 expression by a SIRT1 SMART small interfering RNA duplex sensitized the >20-fold resistant CP-r cells to cisplatin treatment 1.5- to 2-fold, and SIRT1 overexpression by SIRT1 cDNA transfection increased cisplatin resistance in cisplatin-sensitive cells by 2- to 3-fold. Our findings therefore suggest that reduced glucose use and altered mitochondrial metabolism mediated by SIRT1 is one of several alterations that contribute to cellular resistance to cisplatin.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / metabolism
  • Adenocarcinoma / pathology
  • Antineoplastic Agents / pharmacology*
  • Carcinoma, Hepatocellular / metabolism
  • Carcinoma, Hepatocellular / pathology*
  • Carcinoma, Squamous Cell / metabolism
  • Carcinoma, Squamous Cell / pathology*
  • Cell Survival / drug effects
  • Cellular Structures / drug effects
  • Cisplatin / pharmacology*
  • Deoxyglucose / metabolism
  • Drug Resistance, Neoplasm*
  • Electron Spin Resonance Spectroscopy
  • Flow Cytometry
  • Fluorescent Antibody Technique
  • Humans
  • Immunoblotting
  • Liver Neoplasms / metabolism
  • Liver Neoplasms / pathology
  • Membrane Potential, Mitochondrial / drug effects
  • Mitochondria / metabolism*
  • Mitochondria / pathology
  • Oxygen Consumption
  • RNA, Small Interfering / pharmacology
  • Sirtuin 1
  • Sirtuins / antagonists & inhibitors
  • Sirtuins / genetics
  • Sirtuins / metabolism*
  • Tumor Cells, Cultured

Substances

  • Antineoplastic Agents
  • RNA, Small Interfering
  • Deoxyglucose
  • SIRT1 protein, human
  • Sirtuin 1
  • Sirtuins
  • Cisplatin