Castell J V, Gómez-Lechón M J, Miranda M A, Morera I M
Centro de Investigación, Hospital La Fe, Valencia, Spain.
J Photochem Photobiol B. 1992 Apr 15;13(1):71-81. doi: 10.1016/1011-1344(92)80041-s.
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.
在这项工作中，研究了两种非甾体抗炎药布替布芬和氟比洛芬的光毒性。两者对光均不稳定，会产生多种光产物，这些光产物被分离并鉴定出来。不同的光产物是通过一种初级光化学机制形成的，该机制涉及羰基α位的C-C键的初始裂解，随后是几个次级过程。使用两种成熟的体外生物学试验评估了异生物素的细胞毒性作用：(a) 培养的成纤维细胞中乳酸脱氢酶和谷氨酸草酰乙酸转氨酶的酶泄漏，以及 (b) 红细胞裂解。在测定的不同浓度下，苄醇导致培养的成纤维细胞大量泄漏。从布替布芬得到的醇是一种对人红细胞有效的裂解剂。其他光产物布替布芬和氟比洛芬对细胞未产生明显的毒性作用。
