Submit Manuscript  

Article Details


Aurones as New Porcine Pancreatic α-Amylase Inhibitors

[ Vol. 16 , Issue. 3 ]

Author(s):

Khashayar Roshanzamir, Elaheh Kashani-Amin, Azadeh Ebrahim-Habibi* and Latifeh Navidpour*   Pages 333 - 340 ( 8 )

Abstract:


Background: Aurones, (Z)-2-benzylidenebenzofuran-3-one derivatives, are naturallyoccurring 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.

Keywords:

α-amylase, aurones, (Z)-2-arylidenebenzofuran-3-ones, isomers, methoxylated, flavonols.

Affiliation:

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176, Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Biosensor Research Center, Endocrinology and Metabolism Molecular-Cellular Sciences Institute, Tehran University of Medical Sciences, Tehran, Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 14176

Graphical Abstract:



Read Full-Text article