A new series of chrysin derivatives as potent non-saccharide ⍺-glucosidase inhibitors
- PMID: 36210594
- DOI: 10.1016/j.fitote.2022.105301
A new series of chrysin derivatives as potent non-saccharide ⍺-glucosidase inhibitors
Abstract
Twenty-three chrysin derivatives were designed and synthesized by alkylation and bromination reactions. Their structures were confirmed by NMR and mass spectrometry, and their in vitro ⍺-glucosidase (AG) inhibitory activity was investigated. Chrysin derivatives except for 3a, 3b, 2q, and 2r, revealed better activity than the reference acarbose with moderate to very strong inhibition against AG. Notably, 2f, 2j, and 4 showed very strong and strong effects on AG ⍺-glucosidase inhibitory activity with IC50 values of 0.08, 3.47, and 2.97 μM, respectively. Simultaneously, enzyme kinetics study indicated that 2f was a competitive-type inhibitor, while 2j and 4 were mixed-type inhibitors.
Keywords: Alkylation; Bromination; Chrysin derivatives; ⍺-Glucosidase inhibitors.
Copyright © 2022 Elsevier B.V. All rights reserved.
Conflict of interest statement
Declaration of Competing Interest The authors declare no conflicts in financial interests.
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