1. Analogues of xanthones--Chalcones and bis-chalcones as α-glucosidase inhibitors and anti-diabetes candidates.
- Author
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Cai CY, Rao L, Rao Y, Guo JX, Xiao ZZ, Cao JY, Huang ZS, and Wang B
- Subjects
- Chalcones pharmacology, Enzyme Inhibitors pharmacology, Hep G2 Cells, Humans, Hypoglycemic Agents pharmacology, Structure-Activity Relationship, Xanthones chemistry, Chalcones chemistry, Enzyme Inhibitors chemistry, Hypoglycemic Agents chemistry, alpha-Glucosidases drug effects
- Abstract
Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as α-glucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards α-glucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good α-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 μM concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line)., (Copyright © 2017 Elsevier Masson SAS. All rights reserved.)
- Published
- 2017
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