Aurones as New Porcine Pancreatic α-Amylase Inhibitors

Author:

Roshanzamir Khashayar1,Kashani-Amin Elaheh2,Ebrahim-Habibi Azadeh2,Navidpour Latifeh1

Affiliation:

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176, Iran

2. Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Abstract

Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturallyoccurring structural isomers of flavones, with promising pharmacological potential. </P><P> Methods: In this study, the structural requirements for the inhibition of porcine pancreatic &#945;- amylase by hydroxylated or methoxylated aurone derivatives were investigated by assessing their in vitro biological activities against porcine pancreatic &#945;-amylase. </P><P> 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. </P><P> Conclusion: It seems that the OH groups in aurones inhibit &#945;-amylase in a manner similar to that of OH groups in flavones and flavonols.

Funder

Research Council of Tehran University of Medical Sciences

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmaceutical Science,Molecular Medicine

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