Phototoxicity of non-steroidal anti-inflammatory drugs: in vitro testing of the photoproducts of Butibufen and Flurbiprofen.

Abstract

In this work, the phototoxicity of two non-steroidal anti-inflammatory drugs, Butibufen and Flurbiprofen, was examined. Both were unstable to light, to give several photoproducts which were isolated and identified. The different photoproducts were formed by a primary photochemical mechanism which involves an initial cleavage of the C-C bond alpha to the carbonyl group, followed by several secondary processes. The cytotoxic effects of the xenobiotics were evaluated using two well-established biological in vitro tests: (a) enzyme leakage lactate dehydrogenase and glutamate-oxaloacetate transaminase from cultured fibroblasts and (b) lysis of red blood cells. The benzylic alcohols caused extensive leakage from cultured fibroblasts at the different concentrations assayed. The alcohol obtained from Butibufen was a potent lytic agent for human red blood cells. The other photoproducts, Butibufen and Flurbiprofen did not produce observable toxic effects on cells.

• Authors: J V Castell, M J Gómez-Lechón, M A Miranda, I M Morera
• Journal: Journal of photochemistry and photobiology. B, Biology (J Photochem Photobiol B) Vol. 13 Issue 1 Pg. 71-81 (Apr 15 1992) ISSN: 1011-1344 [Print] Switzerland
• PMID: 1403370 (Publication Type: Journal Article)

Chemical References

• Anti-Inflammatory Agents, Non-Steroidal
• Phenylbutyrates
• Radiation-Sensitizing Agents
• Flurbiprofen
• butibufen

Topics

• 3T3 Cells
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (pharmacology, radiation effects)
• Cell Survival (drug effects)
• Erythrocytes (drug effects)
• Fibroblasts (cytology, drug effects)
• Flurbiprofen (pharmacology, radiation effects)
• Hemolysis (drug effects)
• Humans
• In Vitro Techniques
• Kinetics
• Light
• Mice
• Phenylbutyrates (pharmacology, radiation effects)
• Radiation-Sensitizing Agents (pharmacology)