Canudas N, Vargas F, Miranda M A
Centro de Quimica, Instituto Venezolano de Investigaciones Cientificas, Caracas, Venezuela.
Arzneimittelforschung. 1996 Jul;46(7):694-7.
Aqueous solutions of the antihyperlipoproteinemic drug bezafibrate (CAS 41859-67-0) are photolabile towards UV-B light under aerobic conditions. Two compounds were isolated and identified spectroscopically as well as by alternative synthesis as the only photoproducts formed. Their formation involves primary cleavage of the aryloxy-carbon bond and decarboxylation followed by hydrogen abstraction or dimerization. Bezafibrate is phototoxic in vitro as indicated by the photohemolysis test. Furthermore bezafibrate photo-sensitizes peroxidation of linoleic acid as monitored by the UV detection of dienic hydroperoxides. Partial inhibition of these processes on addition of butylated hydroxyanisole (BHA), reduced glutathione (GSH), sodium azide (NaN3) or 1,4-diazabicyclo [2.2.2] octane (DABCO) suggests the involvement of type I as well as type II mechanisms.
抗高脂蛋白血症药物苯扎贝特（CAS 41859-67-0）的水溶液在有氧条件下对UV-B光不稳定。通过光谱分析以及通过替代合成分离并鉴定了两种化合物，它们是形成的唯一光产物。它们的形成涉及芳氧基-碳键的初级裂解和脱羧，然后是氢提取或二聚化。如光溶血试验所示，苯扎贝特在体外具有光毒性。此外，通过二烯氢过氧化物的UV检测监测，苯扎贝特可使亚油酸的过氧化光致敏。加入丁基化羟基茴香醚（BHA）、还原型谷胱甘肽（GSH）、叠氮化钠（NaN3）或1,4-二氮杂双环[2.2.2]辛烷（DABCO）对这些过程的部分抑制表明涉及I型和II型机制。
