Pronounced radiosensitization of cultured human cancer cells by COX inhibitor under acidic microenvironment

Int J Radiat Oncol Biol Phys. 2002 Aug 1;53(5):1314-8. doi: 10.1016/s0360-3016(02)02889-4.

Abstract

Purpose: To demonstrate the influence of pH on the cytotoxicity and radiosensitization by COX (cyclooxygenase) -1 and -2 inhibitors using established human cancer cells in culture.

Methods and materials: Nonselective COX inhibitor, ibuprofen (IB), and selective COX-2 inhibitor, SC-236, were used to determine the cytotoxicity and radiosensitization at varying pH of culture media. Human colon carcinoma cell line (HT-29) was exposed to the drug alone and in combination with radiation at different pH of the cell culture media. The end point was clonogenic ability of the single-plated cells after the treatment.

Results: Cytotoxicity and radiosensitization of IB increased with higher drug concentration and longer exposure time. The most significant radiosensitization was seen with IB (1.5 mM) for 2-h treatment at pH 6.7 before irradiation. The dose-modifying factor as defined by the ratio of radiation doses required to achieve the same effect on cell survival was 1.8 at 10% survival level. In contrast, SC-236 (50 microM for 2-8 h) showed no pH-dependent cytotoxicity. There was modest increase in the cell killing at lower doses of radiation.

Conclusion: An acidic pH was an important factor affecting the increased cytotoxicity and radiosensitization by ibuprofen. Radiation response was enhanced at shoulder portion of the cell survival curve by selective COX-2 inhibitor.

Publication types

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

MeSH terms

  • Cell Survival
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Humans
  • Hydrogen-Ion Concentration
  • Ibuprofen / pharmacology
  • Isoenzymes / antagonists & inhibitors*
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases
  • Pyrazoles / pharmacology
  • Radiation-Sensitizing Agents / pharmacology
  • Sulfonamides / pharmacology
  • Time Factors
  • Tumor Cells, Cultured

Substances

  • 4-(5-(4-chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Isoenzymes
  • Membrane Proteins
  • Pyrazoles
  • Radiation-Sensitizing Agents
  • Sulfonamides
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • PTGS1 protein, human
  • PTGS2 protein, human
  • Prostaglandin-Endoperoxide Synthases
  • Ibuprofen