Literature DB >> 20857221

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

Mahmoud Najafian1, Azadeh Ebrahim-Habibi, Nastaran Hezareh, Parichehreh Yaghmaei, Kazem Parivar, Bagher Larijani.   

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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Year:  2010        PMID： 20857221     DOI： 10.1007/s11033-010-0271-3

Source DB:  PubMed          Journal:  Mol Biol Rep        ISSN： 0301-4851            Impact factor:   2.316


  17 in total

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Authors:  Octávio L Franco; Daniel J Rigden; Francislete R Melo; Maria F Grossi-De-Sá
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Journal:  Biochem J       Date:  2000-02-15       Impact factor: 3.857

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4.  Effect of acarbose (alpha-glucosidase inhibitor) on disaccharase activity in small intestine in KK-Ay and ddY mice.

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5.  Inhibition of alpha-glucosidase and alpha-amylase by flavonoids.

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Journal:  J Nutr Sci Vitaminol (Tokyo)       Date:  2006-04       Impact factor: 2.000

6.  Inhibition of postprandial hyperglycemia by acarbose is a promising therapeutic strategy for the treatment of patients with the metabolic syndrome.

Authors:  S Yamagishi; K Nakamura; M Takeuchi
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Authors:  Chris A Tarling; Kate Woods; Ran Zhang; Harry C Brastianos; Gary D Brayer; Raymond J Andersen; Stephen G Withers
Journal:  Chembiochem       Date:  2008-02-15       Impact factor: 3.164

8.  Flavonoids for controlling starch digestion: structural requirements for inhibiting human alpha-amylase.

Authors:  Elena Lo Piparo; Holger Scheib; Nathalie Frei; Gary Williamson; Martin Grigorov; Chieh Jason Chou
Journal:  J Med Chem       Date:  2008-05-29       Impact factor: 7.446

9.  Human salivary alpha-amylase Trp58 situated at subsite -2 is critical for enzyme activity.

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Journal:  Eur J Biochem       Date:  2004-06

Review 10.  Structure and function of enzymes involved in the biosynthesis of phenylpropanoids.

Authors:  J-L Ferrer; M B Austin; C Stewart; J P Noel
Journal:  Plant Physiol Biochem       Date:  2007-12-31       Impact factor: 4.270
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  11 in total

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2.  Theoretical study on the antioxidant properties of 2'-hydroxychalcones: H-atom vs. electron transfer mechanism.

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4.  Apigenin isolated from A. americana encodes Human and Aspergillus oryzae S2 α-amylase inhibitions: credible approach for antifungal and antidiabetic therapies.

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5.  Gedunin and Azadiradione: Human Pancreatic Alpha-Amylase Inhibiting Limonoids from Neem (Azadirachta indica) as Anti-Diabetic Agents.

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Journal:  PLoS One       Date:  2015-10-15       Impact factor: 3.240

6.  Chalcones, semicarbazones and pyrazolines as inhibitors of cathepsins B, H and L.

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Journal:  Int J Biol Macromol       Date:  2015-07-18       Impact factor: 6.953

Review 7.  Modeling and simulation in medical sciences: an overview of specific applications based on research experience in EMRI (Endocrinology and Metabolism Research Institute of Tehran University of Medical Sciences).

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8.  Synthesis of novel inhibitors of α-amylase based on the thiazolidine-4-one skeleton containing a pyrazole moiety and their configurational studies.

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9.  Reflection on design and testing of pancreatic alpha-amylase inhibitors: an in silico comparison between rat and rabbit enzyme models.

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10.  Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some N-Substituted-4-Phenothiazine-Chalcones.

Authors:  Thai-Son Tran; Minh-Tri Le; Thi-Cam-Vi Nguyen; The-Huan Tran; Thanh-Dao Tran; Khac-Minh Thai
Journal:  Molecules       Date:  2020-08-27       Impact factor: 4.411
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