生物素衍生化环孢素A的合成及其与人亲环素A的相互作用研究  

Synthesis of Biotinylated Cyclosporin A and Studies on Its Interaction with Human Cyclophilin A

作　　者：江辉[1] 麻锦彪[1] 朱向明[1] 惠永正[1] 吴厚铭[1] 陈海宝[1] 

机构地区：[1]中国科学院上海有机化学研究所

出　　处：《化学学报》2001年第10期1745-1750,共6页Acta Chimica Sinica

基　　金：中国科学院知识创新工程项目，中国科学院科研项目，上海市科技发展基金

摘　　要：通过ε-氨基己酸二聚体的乙酯与生物素缩合将其羧端延伸14个原子,然后与氨基衍生化的环孢素A缩合合成了生物素衍生化的环孢素A.经过药物免疫印迹和表面等离子体共振(Surface Plasmon Resonance)测定表明生物素衍生化的环孢素A还保留了与人亲环素A结合的活力.Biotinylated cyclosporin A was synthesized by condensing the amino - derivative of cyclosporin A with ethyl N - ( N - biotinyl - epsilon - aminocapronyl) - epsilon - aminocaproate, which was preformed from coupling biotin and the ethyl ester of dimeric epsilon - aminocaproic acid to extend the carboxyl group of biotin for 14 atoms. Both of drug western blot and surface plasmon resonance (SPR) proved that the biotinylated cyclosporin A remained the capacity of binding human cyclophilin A.

关 键 词：环孢素A 生物素-亲和素系统 人亲环素A 药物免疫印迹 表面等离子体共振 相互作用 免疫抑制剂 

分 类 号：R962[医药卫生—药理学] R979.5[医药卫生—药学]