Cordycepin induces S phase arrest and apoptosis in human gallbladder cancer cells

Molecules. 2014 Jul 31;19(8):11350-65. doi: 10.3390/molecules190811350.

Abstract

Gallbladder cancer is the most common malignant tumor of the biliary tract, and this condition has a rather dismal prognosis, with an extremely low five-year survival rate. To improve the outcome of unresectable and recurrent gallbladder cancer, it is necessary to develop new effective treatments and drugs. The purpose of the present study was to evaluate the effects of cordycepin on human gallbladder cells and uncover the molecular mechanisms responsible for these effects. The Cell Counting Kit-8 (CCK-8) and colony formation assays revealed that cordycepin affected the viability and proliferation of human gallbladder cancer cells in a dose- and time-dependent manner. Flow cytometric analysis showed that cordycepin induced S phase arrest in human gallbladder cancer cell lines(NOZ and GBC-SD cells). Cordycepin-induced apoptosis was observed using an Annexin V/propidium iodide (PI) double-staining assay, and the mitochondrial membrane potential (ΔΨm) decreased in a dose-dependent manner. Additionally, western blot analysis revealed the upregulation of cleaved-caspase-3, cleaved-caspase-9, cleaved-PARP and Bax and the downregulation of Bcl-2, cyclin A and Cdk-2 in cordycepin-treated cells. Moreover, cordycepin inhibited tumor growth in nude mice bearing NOZ tumors. Our results indicate that this drug may represent an effective treatment for gallbladder carcinoma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects*
  • Caspase 3 / genetics
  • Caspase 3 / metabolism
  • Cell Cycle Proteins / genetics
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Deoxyadenosines / chemistry
  • Deoxyadenosines / pharmacology*
  • Disease Models, Animal
  • Gallbladder Neoplasms / genetics
  • Gallbladder Neoplasms / metabolism
  • Gallbladder Neoplasms / pathology
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • Membrane Potential, Mitochondrial / drug effects
  • Mice
  • Molecular Structure
  • Proto-Oncogene Proteins c-bcl-2 / genetics
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • S Phase Cell Cycle Checkpoints / drug effects*
  • Tumor Burden / drug effects
  • Tumor Stem Cell Assay
  • Xenograft Model Antitumor Assays

Substances

  • Antineoplastic Agents
  • Cell Cycle Proteins
  • Deoxyadenosines
  • Proto-Oncogene Proteins c-bcl-2
  • Caspase 3
  • cordycepin