摘要/Abstract
以葡萄糖为原料经多步反应合成了脱氧野尻霉素类两亲化合物FA-DNJ-C6，通过表面张力实验、动态光散射实验（DLS）和透射电镜（TEM）等研究了FA-DNJ-C6的自组装行为，FA-DNJ-C6在水溶液中形成稳定的超分子自组装体.经酶抑制实验研究了FA-DNJ-C6自组装体的糖苷酶抑制活性，进而发现FA-DNJ-C6自组装体对α-糖苷酶具有好的选择性，尤其是对α-甘露糖苷酶，其抑制活性的Ki值为（0.107±0.021）μmol/L，与阳性对照（米格列醇）相比，活性提高了339倍，这主要是由于α-甘露糖苷酶具有多个识别位点的空腔，可发挥多效价协同增强的键合作用，提高糖苷酶抑制活性.
关键词: 糖苷酶抑制剂, 自组装, 多效价, 1-脱氧野尻霉素
An amphiphilic derivative FA-DNJ-C6 with deoxynojirimycin modification was synthesized. The self-assembly behavior of FA-DNJ-C6 was studied by a surface tension test, dynamic light scattering test (DLS) and transmission electron microscopy (TEM). FA-DNJ-C6 formed stable supramolecular self-assembly in aqueous solution. Furthermore, the glycosidase inhibition activities of FA-DNJ-C6 were studied. FA-DNJ-C6 as multivalent glycosidase inhibitor showed potent glycosidase effect against α-mannosidase with Ki value of (0.107±0.021) μmol/L, an increase of approximately 339-fold compared with the control drug of miglitol, which was due to the multivalent binding sites in α-mannosidase.
Key words: glycosidase inhibitor, self-assembly, multivalent, 1-deoxynojirimycin
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