Vohl M L, Westarp M E, Wekerle H, Gerlach M, Jutzi P, Przuntek H
Neurologische Universitätsklinik Würzburg.
Arzneimittelforschung. 1990 Jan;40(1):80-4.
The therapeutic effects of mercaptopurine (6-mercaptopurine, 6-MP) and a silylated derivative (6-trimethylsilylthio-9-trimethyl-silylpurine, S-MP) were compared on the course of T lymphocyte line mediated experimental allergic encephalomyelitis (t-EAE). This transferred EAE is a passively induced model disease in Lewis rats easy to elicit, reliably reproducible and characterized by a dose-dependent lethality. If given at different points in single injections the silicon derivative is shown to be more efficient than 6-MP (43/125 surviving animals compared to 26/129), severity of disease is attenuated and number of survivors increased. Silylation is able to improve blood-brain barrier and cellular permeability; S-MP suppresses intrathecal inflammatory cells more effectively than the original immunosuppressant.
比较了巯嘌呤（6-巯基嘌呤，6-MP）和一种硅烷化衍生物（6-三甲基硅硫基-9-三甲基硅嘌呤，S-MP）对T淋巴细胞系介导的实验性变应性脑脊髓炎（t-EAE）病程的治疗效果。这种转移性EAE是在Lewis大鼠中被动诱导的模型疾病，易于引发，可可靠重现，且具有剂量依赖性致死性。单次注射时，若在不同时间点给药，硅烷化衍生物比6-MP更有效（存活动物为43/125，而6-MP为26/129），疾病严重程度减轻，存活动物数量增加。硅烷化能够改善血脑屏障和细胞通透性；S-MP比原始免疫抑制剂更有效地抑制鞘内炎症细胞。
