Molecular Biology Reports 2011-03-01

Trans-chalcone: a novel small molecule inhibitor of mammalian alpha-amylase.

Mahmoud Najafian, Azadeh Ebrahim-Habibi, Nastaran Hezareh, Parichehreh Yaghmaei, Kazem Parivar, Bagher Larijani

Index: Mol. Biol. Rep. 38(3) , 1617-20, (2011)

Full Text: HTML

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.

Related Compounds

  • (E)-Chalcone
  • Scutellarein

Related Articles:

Impact of induced fit on ligand binding to the androgen receptor: a multidimensional QSAR study to predict endocrine-disrupting effects of environmental chemicals.

2005-09-08

[J. Med. Chem. 48 , 5666-74, (2005)]

A chemical screening approach reveals that indole fluorescence is quenched by pre-fibrillar but not fibrillar amyloid-beta.

2009-09-01

[Bioorg. Med. Chem. Lett. 19 , 4952-7, (2009)]

Novel chalcone derivatives as potent Nrf2 activators in mice and human lung epithelial cells.

2011-06-23

[J. Med. Chem. 54 , 4147-59, (2011)]

Antimycobacterial and anti-inflammatory activities of substituted chalcones focusing on an anti-tuberculosis dual treatment approach.

2015-01-01

[Molecules 20 , 8072-93, (2015)]

Fluorinated 2'-hydroxychalcones as garcinol analogs with enhanced antioxidant and anticancer activities.

2010-10-01

[Bioorg. Med. Chem. Lett. 20 , 5818-21, (2010)]

More Articles...