<Emphasis Type="Italic">Trans</Emphasis>-chalcone: a novel small molecule inhibitor of mammalian alpha-amylase |
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| Authors: | Mahmoud Najafian Azadeh Ebrahim-Habibi Nastaran Hezareh Parichehreh Yaghmaei Kazem Parivar Bagher Larijani |
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| Institution: | (1) Science and Research Branch Islamic Azad University, Tehran, Iran;(2) Endocrinology and Metabolism Research Center, Tehran University of Medical Sciences, Tehran, Iran; |
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| Abstract: | Trans-chalcone (1,3-diphenyl-2-propen-1-one), a biphenolic core structure of flavonoids precursor was tested for inhibitory activity
toward alpha-amylase. Porcine pancreatic alpha-amylase was observed to be effectively inhibited by this compound, which showed
competitive behavior with a K
i
of 48 μM. Soluble starch (the natural substrate of the enzyme) was used in this study in order to obtain more realistic results.
The possible binding mode of the compound was assessed in silico, and the two residues Trp59, and Tyr62 were proposed as main interacting residues with trans-chalcone. In conclusion, this compound could be used to design effective inhibitors of alpha-amylase. |
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