Phototoxic properties of quinine and quinidine: two quinoline methanol isomers.

Photo-dermatology Pub Date : 1988-06-01
B Ljunggren, L E Wirestrand
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Abstract

Clinical photoreactions have been reported for quinine and quinidine after systemic and topical administration. We have investigated the phototoxic properties of these two quinoline methanol isomers in vitro using the Candida albicans inhibition test and photohemolysis, and in vivo with the mouse tail phototoxicity test. Both isomers were phototoxic in the hemolysis model, quinine being the more potent compound. In the Candida test only quinidine was phototoxically active. In the mouse tail model, measuring edema, the phototoxic activity of quinidine was comparatively low, causing a 7.3% wet weight increase of tail tissue at a dose of 150 mg/kg intraperitoneally of drug and 54 J/cm2 of UVA. In spite of its structural similarity to quinidine, quinine was not phototoxic in the mouse. These studies support the assumption, based on clinical data, that quinine photoreactions probably have a non-phototoxic mechanism. For quinidine, however, light-induced reactions based on phototoxicity can not be ruled out, since low-grade phototoxic properties were demonstrated in vivo.

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奎宁和奎尼丁的光毒性:两种喹啉甲醇异构体。
奎宁和奎尼丁在全身和局部给药后均有临床光反应的报道。我们利用体外白色念珠菌抑制试验和光溶血试验研究了这两种喹啉甲醇异构体的光毒性,在体内用小鼠尾光毒性试验研究了它们的光毒性。在溶血模型中,两种异构体都具有光毒性,奎宁是更有效的化合物。在念珠菌试验中,只有奎尼丁具有光毒性。在小鼠尾部模型中,测量水肿,奎尼丁的光毒活性相对较低,在150 mg/kg的腹腔给药剂量和54 J/cm2的UVA剂量下,导致尾组织湿重增加7.3%。尽管其结构与奎宁相似,但奎宁对小鼠没有光毒性。这些研究支持了基于临床数据的假设,即奎宁光反应可能具有非光毒性机制。然而,对于奎尼丁,不能排除基于光毒性的光诱导反应,因为在体内证明了低等级的光毒性。
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