Jennings F W, Atouguia J M, Murray M
Department of Veterinary Parasitology, University of Glasgow, UK.
Acta Trop. 1996 Oct;62(2):83-9. doi: 10.1016/s0001-706x(96)00036-8.
Both melarsomine dichlorhydrate (mel Cy, Cymelarsan) and melarsen oxide can be dissolved in dimethylsulfoxide and converted into a gel by the addition of hydroxypropylcellulose. When Trypanosoma brucei brucei-infected mice are treated topically with these gels the circulating trypanosomes are rapidly cleared from the circulation but the infections relapse soon after the last application. However, when these two compounds are allowed to react with 2,3-dimercaptopropinol (British anti-lewisite, BAL) and form "melarsoprol" their efficacy, especially in the case of mel Cy, is restored to that of commercial melarsoprol (Arsobal) and trypanosomes in the central nervous system (CNS) can be eliminated. This would indicate that the dimercaptopropinol portion of the molecule does not act solely as an "antidote" to arsenic toxicity, but also plays an important role in the absorption of melarsoprol through the skin and/or blood-brain barrier into the CNS and/or into the trypanosome.
二盐酸美拉胂醇（美拉胂醇，Cymelarsan）和氧化美拉胂均可溶于二甲基亚砜，并通过添加羟丙基纤维素转化为凝胶。当用这些凝胶局部治疗感染布氏布氏锥虫的小鼠时，循环中的锥虫会迅速从循环中清除，但在最后一次用药后不久感染就会复发。然而，当这两种化合物与2,3 - 二巯基丙醇（英国抗路易氏剂，BAL）反应形成“美拉胂醇”时，它们的疗效，尤其是美拉胂醇的疗效，恢复到了商业美拉胂醇（Arsobal）的水平，并且中枢神经系统（CNS）中的锥虫可以被清除。这表明分子中的二巯基丙醇部分不仅作为砷毒性的“解毒剂”起作用，而且在美拉胂醇通过皮肤和/或血脑屏障吸收进入中枢神经系统和/或锥虫中也起着重要作用。
