Simvastatin Strongly Augments Proapoptotic, Anti-inflammatory and Cytotoxic Activity of Oxicam Derivatives in Doxorubicin-resistant Colon Cancer Cells

Anticancer Res. 2019 Feb;39(2):727-734. doi: 10.21873/anticanres.13169.

Abstract

Background: Incidence of cancer is still increasing. Chemotherapy is often unsuccessful; moreover, anticancer drugs cause serious side-effects. It is necessary to develop effective agents for combination therapies that would increase antitumor effects of treatment and reduce its side-effects.

Materials and methods: Anticancer activity of oxicam derivatives (PR17 and PR18) alone and in combination with simvastatin on doxorubicin-resistant colon cancer cells was studied. Apoptosis was investigated via caspase-3 activation assay as well as via western blot analysis of expression of apoptotic components, B-cell lymphoma 2 protein (BCL2) and BCL2-associated X protein (BAX). Expression and activity of cyclo-oxygenase-2 (COX2) was also assessed.

Results: Oxicam derivatives induced apoptosis through a caspase-3-dependent pathway, up-regulated BAX expression, and down-regulated BCL2 expression. Additionally, oxicam derivatives reduced expression and activity of COX2. Effect of oxicam derivatives on these processes was strongly potentiated by simvastatin.

Conclusion: Oxicam derivatives at low concentrations effectively inhibit growth of cancer cells after co-administration with simvastatin.

Keywords: Oxicam derivatives; apoptosis; cancer combination therapy; cyclo-oxygenase-2; simvastatin.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Apoptosis*
  • Caspase 3 / metabolism
  • Cell Line, Tumor
  • Cell Survival
  • Colonic Neoplasms / pathology*
  • Cyclic S-Oxides / chemistry
  • Cyclic S-Oxides / pharmacology*
  • Cyclooxygenase 2 / metabolism
  • Doxorubicin / pharmacology*
  • Drug Resistance, Neoplasm*
  • Drug Synergism
  • Enzyme Activation
  • Humans
  • Inhibitory Concentration 50
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • Simvastatin / pharmacology*
  • Thiazines / chemistry
  • Thiazines / pharmacology*
  • Up-Regulation
  • bcl-2-Associated X Protein / metabolism

Substances

  • Antineoplastic Agents
  • BAX protein, human
  • BCL2 protein, human
  • Cyclic S-Oxides
  • Proto-Oncogene Proteins c-bcl-2
  • Thiazines
  • bcl-2-Associated X Protein
  • oxicam PR18
  • Doxorubicin
  • Simvastatin
  • Cyclooxygenase 2
  • PTGS2 protein, human
  • CASP3 protein, human
  • Caspase 3