A3 adenosine receptor-mediated p53-dependent apoptosis in Lu-65 human lung cancer cells

Cell Physiol Biochem. 2012;30(1):210-20. doi: 10.1159/000339058. Epub 2012 Jun 19.

Abstract

Background/aims: A(3) adenosine receptor mediates apoptosis in cancer cells via diverse signaling pathways. The present study examined A(3) adenosine receptor-mediated apoptosis in Lu-65 cells, a human giant cell lung carcinoma cell line.

Methods: MTT assay, TUNEL staining, real-time RT-PCR, Western blotting, and assay of caspase-3, -8, and -9 activities were carried out in Lu-65 cells, and A(3) adenosine receptor or p53 was knocked-down by transfecting each siRNA into cells.

Results: Extracellular adenosine induces Lu-65 cell apoptosis in a concentration (0.01-10 mM)-dependent manner, and the effect was inhibited by the A(3) adenosine receptor inhibitor MRS1191 or by knocking-down A(3) adenosine receptor or p53. Like adenosine, the A(3) adenosine receptor agonist 2-Cl-IB-MECA also induced Lu-65 cell apoptosis. Adenosine upregulated expression of p53 and Noxa mRNAs and activated caspase-3 and -9, but not caspase-8. Those adenosine effects were still inhibited by knocking-down A(3) adenosine receptor or p53.

Conclusion: The results of the present study show that adenosine upregulates p53 expression via A(3) adenosine receptor, to promote p53-dependent Noxa gene transcription, causing activation of caspase-9 and the effector caspase-3 to induce Lu-65 cell apoptosis.

MeSH terms

  • Adenosine / analogs & derivatives
  • Adenosine / pharmacology
  • Adenosine / physiology
  • Adenosine A3 Receptor Agonists / pharmacology
  • Adenosine A3 Receptor Antagonists / pharmacology
  • Apoptosis*
  • Caspases / metabolism
  • Cell Line, Tumor
  • Cell Survival
  • Dihydropyridines / pharmacology
  • Enzyme Activation
  • Gene Expression Regulation
  • Gene Knockdown Techniques
  • Humans
  • Lung Neoplasms
  • Proto-Oncogene Proteins c-bcl-2 / genetics
  • Proto-Oncogene Proteins c-bcl-2 / metabolism
  • RNA Interference
  • Receptor, Adenosine A3 / genetics
  • Receptor, Adenosine A3 / metabolism*
  • Tumor Suppressor Protein p53 / genetics
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • Adenosine A3 Receptor Agonists
  • Adenosine A3 Receptor Antagonists
  • Dihydropyridines
  • MRS 1191
  • PMAIP1 protein, human
  • Proto-Oncogene Proteins c-bcl-2
  • Receptor, Adenosine A3
  • TP53 protein, human
  • Tumor Suppressor Protein p53
  • Caspases
  • Adenosine
  • 2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide