Synthesis of N-dialkylphosphoryl iminosugar derivatives and their immunosuppressive activities.
Synthesis of N-dialkylphosphoryl iminosugar derivatives and their immunosuppressive activities.
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DOI：
10.1039/c5ob01278c
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发表时间：
2015-09
影响因子：
3.2
通讯作者：
Xue-Yan Yang;Decai Xiong;Chengcheng Song;G. Tai;X. Ye
中科院分区：
文献类型：
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作者：
Xue-Yan Yang;Decai Xiong;Chengcheng Song;G. Tai;X. Ye
合成了12种新型N-二烷基磷酸亚氨基糖衍生物，并评估了它们对小鼠脾细胞增殖以及IFN-γ和IL-4分泌的免疫抑制活性。实验数据表明，具有双长烷基链的亚氨基糖比具有单长烷基链的亚氨基糖表现出更好的免疫抑制作用，其中具有10个碳直链烷基链的亚氨基糖表现出最强的免疫抑制活性。细胞因子分泌的测定表明，在亚氨基糖上引入二烷基链可以通过改变烷基链的长度来调节免疫抑制的极化。构效关系的揭示可能有利于亚氨基糖的结构修饰以寻找新型免疫抑制剂。
Twelve novel N-dialkylphosphoryliminosugar derivatives were synthesized and their immunosuppressive activities were evaluated on the proliferation of the mouse splenocytes and the secretion of IFN-γ and IL-4. The experimental data demonstrated that the iminosugars with the double long alkyl chains exhibited better inhibitory effects than those with the single long alkyl chain, and the iminosugars with the 10-carbon linear alkyl chain exhibited the strongest immunosuppressive activities. The assay of the cytokine secretion showed that the introduction of dialkyl chains on iminosugars could regulate the polarization of immune inhibition by varying the length of the alkyl chains. The disclosure of the structure-activity relationships may benefit the structural modifications of iminosugars to find new types of immunosuppressive agents.