Synthesis, self-assembly behaviours and multivalent glycosidase inhibition effects of a deoxynojirimycin modified perylene bisimide derivative.

J Mater Chem B

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.

Published: February 2019

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.

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http://dx.doi.org/10.1039/c8tb03122cDOI Listing

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