Viola G, Miolo G, Vedaldi D, Dall'Acqua F
Department of Pharmaceutical Sciences, University of Padua, Italy.
Farmaco. 2000 Mar;55(3):211-8. doi: 10.1016/s0014-827x(99)00116-0.
Amitriptyline and imipramine, two tricyclic antidepressant drugs, have been studied to evaluate their phototoxic potential using various models. Reactive oxygen species production was investigated. A negligible production of singlet oxygen was observed for both compounds whereas a significant production of superoxide anion was noted for amitriptyline in particular. Moderate red blood cell lysis under UVA light (365 nm) was induced in the presence of the two drugs at a concentration of 50 microM. Cellular phototoxicity was investigated on a murine fibroblast cell line (3T3). The two drugs were phototoxic causing cell death at a concentration of 100 microM and a UVA dose in the range of 3.3-6.6 J/cm2. Furthermore, the two drugs photosensitized the peroxidation of linoleic acid, as monitored by the formation of dienic hydroperoxides. The presence of BHA and GSH, two free radical scavengers, significantly reduced the lipid oxidation photoinduced by the drugs, suggesting a predominant involvement of radical species. Finally, the involvement of nucleic acids in the phototoxicity mechanism was also investigated using a pBR322 plasmid DNA as a model.
已使用多种模型对两种三环类抗抑郁药物阿米替林和丙咪嗪的光毒性潜力进行了研究。对活性氧的产生进行了调查。两种化合物均观察到单线态氧的产生可忽略不计,而尤其对于阿米替林,超氧阴离子的产生显著。在浓度为50微摩尔的这两种药物存在下,UVA光(365纳米)诱导了中度红细胞裂解。在小鼠成纤维细胞系(3T3)上研究了细胞光毒性。这两种药物具有光毒性,在浓度为100微摩尔且UVA剂量在3.3 - 6.6焦每平方厘米范围内时会导致细胞死亡。此外,这两种药物使亚油酸过氧化光敏化,通过二烯氢过氧化物的形成进行监测。两种自由基清除剂丁基羟基茴香醚(BHA)和谷胱甘肽(GSH)的存在显著降低了药物光诱导的脂质氧化,表明自由基物种起主要作用。最后,还使用pBR322质粒DNA作为模型研究了核酸在光毒性机制中的作用。