Aurones As New Porcine Pancreatic Α-Amylase Inhibitors Publisher



Roshanzamir K¹ ; Kashaniamin E^{2, 3} ; Ebrahimhabibi A^{2, 3} ; Navidpour L¹ Show Affiliations
Source: Letters in Drug Design and Discovery Published:2019

Abstract

Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturally-occurring structural isomers of flavones, with promising pharmacological potential. Methods: In this study, the structural requirements for the inhibition of porcine pancreatic α-amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic α-amylase. Results: The structure-activity relationship of these inhibitors based on both in vitro and in silico findings showed that the hydrogen bonds between the OH groups of the A or B ring of (Z)-benzylidenebenzofuran-3-one derivatives and the catalytic residues of the binding site are crucial for their inhibitory activities. Conclusion: It seems that the OH groups in aurones inhibit α-amylase in a manner similar to that of OH groups in flavones and flavonols. © 2019 Bentham Science Publishers.