Synthesis and Immunomodulating Activity of New Analogues of Fingolimod
Synthesis and Immunomodulating Activity of New Analogues of Fingolimod
复制标题
芬戈莫德新类似物的合成及其免疫调节活性
DOI：
10.1002/ardp.201100092
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发表时间：
2012-02-01
影响因子：
5.1
通讯作者：
Lu, Wei
中科院分区：
文献类型：
--
作者：
Feng, Xiang-Jun;Yang, Xiao-Ying;Lu, Wei
用反式-4-烷基取代环己烷取代Fingolimod的柔性C8烷基链，合成了5个新的免疫调节剂1a-1 e。对于体外试验，将化合物溶解在DMSO中作为储备溶液，并用RPMI 1640营养液稀释至所需浓度。对于体内试验，在含有0.5%DMSO的无病原体盐水中制备化合物。这些新的免疫调节剂显示出更强的体外免疫抑制活性和适度的体内免疫调节活性。它们显示对DNFB诱导的DTH反应的治疗作用和对抗原特异性T细胞增殖的抑制作用。
Five new immunomodulators 1a-1e by using a trans-4-alkyl-substituted cyclohexane to replace the flexible C8 alkyl chain of Fingolimod were synthesized. For in-vitro test, the compounds were dissolved in DMSO as a stock solution and diluted to a desired concentration with RPMI 1640 nutrient solution. For in-vivo test, the compounds were prepared in pathogen-free saline containing 0.5% DMSO. These new immunomodulators displayed more potent immunoinhibitory activities in vitro and moderate immunomodulating activities in vivo. They show therapeutic effects on DNFB-induced DTH reaction and inhibitory effects on the antigen-specific T-cell proliferation.