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Supramolecular azasugar clusters based on an amphiphilic fatty-acid-deoxynojirimycin derivative as multivalent glycosidase inhibitors

Author:
Li, Min, Wang, Ke-Rang, Yang, Jian-Xing, Peng, Ya-Tong, Liu, Yi-Xuan, Zhang, Hong-Xin, Li, Xiao-Liu
Source:
Journal of materials chemistry B 2019 v.7 no.9 pp. 1379-1383
ISSN:
2050-7518
Subject:
alpha-mannosidase, deoxynojirimycin, enzyme inhibitors, glycemic effect, mice, pH
Abstract:
A novel supramolecular multivalent glycosidase inhibitor was constructed based on the amphiphilic deoxynojirimycin derivative FA-DNJ. FA-DNJ self-assembled into spherical assemblies with the diameters between 103 nm and 137 nm under different pH values (pH 2–7) and showed a potent glycosidase effect against α-mannosidase with a Kᵢ value of 0.11 μM, an effect that increased approximately 330-fold compared with that of miglitol. In addition, FA-DNJ exhibited a hypoglycaemic effect in mice.
Agid:
6322500