脱氧野尻霉素修饰的苝二酰亚胺衍生物的合成、自组装行为及多价糖苷酶抑制作用。
Synthesis, self-assembly behaviours and multivalent glycosidase inhibition effects of a deoxynojirimycin modified perylene bisimide derivative.
机构信息
Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Key Laboratory of Chemical Biology of Hebei Province, College of Chemistry and Environmental Science, Hebei University, Baoding 071002, China.
出版信息
J Mater Chem B. 2019 Feb 28;7(8):1270-1275. doi: 10.1039/c8tb03122c. Epub 2019 Jan 31.
A self-assembled multivalent glycosidase inhibitor based on perylene bisimide-deoxynojirimycin conjugates was constructed, inhibited α-mannosidase and exhibited a K value of 38 nM, increased approximately 2763-fold compared with the control drug (miglitol). Furthermore, the postprandial blood glucose (PBG) level in mice of PBI-DNJ was firstly studied. PBI-DNJ exhibited a hypoglycaemic effect in vivo. Importantly, this work developed a new means to explore the hypoglycaemic effect in mice based on self-assembled glycosidase inhibitors.
基于苝二酰亚胺-去氧野尻霉素偶联物构建了一种自组装的多价糖苷酶抑制剂，该抑制剂抑制 α-甘露糖苷酶，其 K 值为 38 nM，与对照药物（米格列醇）相比，增加了约 2763 倍。此外，首次研究了 PBI-DNJ 对小鼠餐后血糖（PBG）水平的影响。PBI-DNJ 在体内具有降血糖作用。重要的是，这项工作为基于自组装糖苷酶抑制剂探索小鼠的降血糖作用提供了一种新方法。
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