Sulindac induces apoptosis, inhibits proliferation and activates caspase-3 in Hep G2 cells

Anticancer Res. 2002 Jan-Feb;22(1A):263-6.

Abstract

Background: It has recently been reported that sulindac has an apoptotic effect on KYN-2 cells, an undifferentiated hepatoma cell line. The present work investigates whether sulindac also has an apoptotic effect on well-differentiated hepatoma cells and what its potential mechanism might be.

Materials and methods: Hep G2 cells were treated with sulindac at different concentrations. Apoptosis rate, cell proliferation and 3H-thymidine incorporation were measured. The activities of caspase-3, acid and neutral sphingomyelinase and the changes of sphingomyelin content were also assayed.

Results: Sulindac dose-dependently induced apoptosis in Hep G2 cells; both sulindac sulfone and sulfide had similar effects. The apoptosis was accompanied by an increase of caspase-3 activity and a decrease of cell proliferation and 3H-thymidine incorporation. No significant change could be observed for the activity of sphingomyelinase and sphingomyelin content.

Conclusion: Sulindac induces apoptosis and inhibits proliferation in Hep G2 cells. The effect may be mediated by a pathway related to caspase-3 activation but independent of sphingomyelin metabolism

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Apoptosis / physiology
  • Carcinoma, Hepatocellular / drug therapy*
  • Carcinoma, Hepatocellular / enzymology
  • Carcinoma, Hepatocellular / pathology
  • Caspase 3
  • Caspases / metabolism*
  • Cell Division / drug effects
  • DNA, Neoplasm / antagonists & inhibitors
  • DNA, Neoplasm / biosynthesis
  • Dose-Response Relationship, Drug
  • Enzyme Activation / drug effects
  • Humans
  • Liver Neoplasms / drug therapy*
  • Liver Neoplasms / enzymology
  • Liver Neoplasms / pathology
  • Sphingomyelin Phosphodiesterase / metabolism
  • Sulindac / analogs & derivatives*
  • Sulindac / pharmacology*
  • Tumor Cells, Cultured

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antineoplastic Agents
  • DNA, Neoplasm
  • Sulindac
  • sulindac sulfide
  • Sphingomyelin Phosphodiesterase
  • CASP3 protein, human
  • Caspase 3
  • Caspases
  • sulindac sulfone