Par-4, a proapoptotic gene, is regulated by NSAIDs in human colon carcinoma cells

Gastroenterology. 2000 Jun;118(6):1012-7. doi: 10.1016/s0016-5085(00)70352-0.

Abstract

Background & aims: Many reports indicate that nonsteroidal anti-inflammatory drugs (NSAIDs) have antineoplastic effects, but the precise molecular mechanism(s) responsible are unclear. We evaluated the effect of cyclooxygenase (COX) inhibitors (NSAIDs) on human colon carcinoma cells (HCA-7) and identified several genes that are regulated after treatment with NS-398, a selective COX-2 inhibitor.

Methods: Differential display polymerase chain reaction cloning techniques were used to identify genes regulated by treatment with NSAIDs and selective COX-2 inhibitors.

Results: A prostate apoptosis response 4 (Par-4) gene was up-regulated after NSAID treatment. Par-4 was first isolated from prostate carcinoma cells undergoing apoptosis, and expression of Par-4 sensitized cancer cells to apoptotic stimuli. Par-4 levels were increased in cells treated with COX inhibitors such as NS-398, nimesulide, SC-58125, and sulindac sulfide. Treatment of HCA-7 cells with these agents also induced apoptotic cell death.

Conclusions: The results suggest that regulation of Par-4 contributes to the proapoptotic effects of high-dose COX inhibitors (NSAIDs) by serving as a downstream mediator leading to initiation of programmed cell death.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Apoptosis / drug effects*
  • Apoptosis / genetics
  • Apoptosis Regulatory Proteins
  • Blotting, Northern
  • Blotting, Western
  • Carrier Proteins / analysis
  • Carrier Proteins / genetics*
  • Colonic Neoplasms
  • Cyclooxygenase Inhibitors / pharmacology
  • DNA Fragmentation
  • Gene Expression / drug effects
  • Gene Expression / physiology
  • Humans
  • Intestinal Mucosa / chemistry
  • Intestinal Mucosa / cytology*
  • Intestinal Mucosa / enzymology
  • Intracellular Signaling Peptides and Proteins*
  • Nitrobenzenes / pharmacology*
  • Protein Kinase C / metabolism
  • Pyrazoles / pharmacology
  • RNA, Messenger / analysis
  • Sulfonamides / pharmacology*
  • Sulindac / analogs & derivatives
  • Sulindac / pharmacology
  • Tumor Cells, Cultured

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Apoptosis Regulatory Proteins
  • Carrier Proteins
  • Cyclooxygenase Inhibitors
  • Intracellular Signaling Peptides and Proteins
  • Nitrobenzenes
  • Pyrazoles
  • RNA, Messenger
  • Sulfonamides
  • prostate apoptosis response-4 protein
  • N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide
  • 1-((4-methylsulfonyl)phenyl)-3-trifluoromethyl-5-(4-fluorophenyl)pyrazole
  • Sulindac
  • sulindac sulfide
  • Protein Kinase C
  • nimesulide