Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents
Design and Synthesis of Marine Phidianidine Derivatives as Potential Immunosuppressive Agents
复制标题
潜在免疫抑制剂海洋菲迪亚啶衍生物的设计与合成
DOI：
10.1021/acs.jmedchem.8b01430
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发表时间：
2018-12-27
影响因子：
7.3
通讯作者：
Li, Xu-Wen
中科院分区：
文献类型：
--
作者：
Liu, Jin;Li, Heng;Li, Xu-Wen
在我们从海洋来源寻找高效低毒的潜在免疫抑制剂过程中，设计、合成了一系列新型海洋菲啶啶衍生物，并对其免疫抑制活性进行了评估。测试了这些化合物对刀豆蛋白A诱导的T细胞和脂多糖诱导的B细胞增殖的抑制活性。化合物14a和18c显示出最有前景的抑制效果且毒性较低，进一步发现它们在纯化的T细胞和B细胞上分别对T细胞受体（TCR）和B细胞受体（BCR）交联具有免疫调节活性。
A series of novel marine phidianidine derivatives were designed, synthesized, and evaluated for their immunosuppressive activities during our search of potential immunosuppressive agents with high efficacy and low toxicity from marine sources. These compounds were tested for their inhibitory activity on Con A induced T cell and lipopolysaccharide-induced B cell proliferation. Compounds 14a and 18c, displaying the most promising inhibitory effects and low toxicities, were further found to possess immune regulatory activities upon cross-linking of T cell receptor (TCR) and B cell receptor (BCR) on purified T and B cells, respectively.