Literature DB >> 32173438

Exploring efficacy of indole-based dual inhibitors for α-glucosidase and α-amylase enzymes: In silico, biochemical and kinetic studies.

Abdel-Nasser Kawde1, Muhammad Taha2, Raneem Saud Alansari3, Noor Barak Almandil4, El Hassane Anouar5, Nizam Uddin6, Fazal Rahim7, Sridevi Chigurupati8, Muhammad Nawaz9, Shawkat Hayat7, Mohamad Ibrahim4, Praveen Kumar Elakurthy10, Venugopal Vijayan11, Mohamed Morsy12, Hossieny Ibrahim13, Nadeem Baig12, Khalid Mohammed Khan14.   

Abstract

α-Glucosidase and α-amylase are enzymes which are associated with diabetic II. These enzymes break macromolecules of sugar into monosugar molecules which is soluble in body, hence increase the sugar level in blood. There is need to develop economical and save inhibitors to prevent them from breaking sugar macromolecules to soluble molecules which will control the level of sugar in blood. Therefore, we synthesized indole-based derivatives (1-18) and evaluated as dual inhibitor for α-glucosidase and α-amylase. These chemical scaffolds were built with variation in aryl ring which were found active with good to moderate activity for α-glucosidase having IC50 value ranging from 13.99 ± 0.10 to 59.09 ± 0.30 μM when compared with standard acarbose with IC50 of 11.29 ± 0.10 μM; for α-amylase IC50 value ranging from 13.14 ± 0.10 to 58.99 ± 0.30 μM when compared with the standard acarbose with IC50 of 11.12 ± 0.10 μM. Structure activity relationship (SAR) has been established for all compounds. Enzymatic kinetic study and molecular docking study have been carried out to investigate the binding interactions α-glucosidase and α-amylase enzyme.
Copyright © 2020 Elsevier B.V. All rights reserved.

Entities:  

Keywords:  Enzymatic kinetic study; Indole; Molecular docking; α-Amylase; α-Glucosidase

Mesh:

Substances:

Year:  2020        PMID: 32173438     DOI: 10.1016/j.ijbiomac.2020.03.090

Source DB:  PubMed          Journal:  Int J Biol Macromol        ISSN: 0141-8130            Impact factor:   6.953


  3 in total

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Journal:  Pharmaceuticals (Basel)       Date:  2022-05-27

2.  Adsorption and desorption characteristics of polyphenols from Eucommia ulmoides Oliv. leaves with macroporous resin and its inhibitory effect on α-amylase and α-glucosidase.

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Journal:  Molecules       Date:  2021-05-04       Impact factor: 4.411

  3 in total

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