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Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship

α-Amylase has been considered an important therapeutic target for the management of type 2 diabetes mellitus (T2DM), decreasing postprandial hyperglycaemia (PPHG). In the present work, a panel of 40 structurally related flavonoids was tested, concerning their ability to inhibit α-amylase activity, u...

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Autores principales: Proença, Carina, Freitas, Marisa, Ribeiro, Daniela, Tomé, Sara M., Oliveira, Eduardo F. T., Viegas, Matilde F., Araújo, Alberto N., Ramos, Maria J., Silva, Artur M. S., Fernandes, Pedro A., Fernandes, Eduarda
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6366418/
https://www.ncbi.nlm.nih.gov/pubmed/30724629
http://dx.doi.org/10.1080/14756366.2018.1558221
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author Proença, Carina
Freitas, Marisa
Ribeiro, Daniela
Tomé, Sara M.
Oliveira, Eduardo F. T.
Viegas, Matilde F.
Araújo, Alberto N.
Ramos, Maria J.
Silva, Artur M. S.
Fernandes, Pedro A.
Fernandes, Eduarda
author_facet Proença, Carina
Freitas, Marisa
Ribeiro, Daniela
Tomé, Sara M.
Oliveira, Eduardo F. T.
Viegas, Matilde F.
Araújo, Alberto N.
Ramos, Maria J.
Silva, Artur M. S.
Fernandes, Pedro A.
Fernandes, Eduarda
author_sort Proença, Carina
collection PubMed
description α-Amylase has been considered an important therapeutic target for the management of type 2 diabetes mellitus (T2DM), decreasing postprandial hyperglycaemia (PPHG). In the present work, a panel of 40 structurally related flavonoids was tested, concerning their ability to inhibit α-amylase activity, using a microanalysis screening system, an inhibitory kinetic analysis and molecular docking calculations. From the obtained results, it was possible to observe that the flavone with a -Cl ion at 3-position of C-ring, an –OH group at 3′- and 4′- positions of B-ring and at 5- and 7- positions of A-ring and the C2 = C3 double bond, was the most active tested flavonoid, through competitive inhibition. In conclusion, some of the tested flavonoids have shown promising inhibition of α-amylase and may be considered as possible alternatives to the modulation of T2DM.
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spelling pubmed-63664182019-02-15 Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship Proença, Carina Freitas, Marisa Ribeiro, Daniela Tomé, Sara M. Oliveira, Eduardo F. T. Viegas, Matilde F. Araújo, Alberto N. Ramos, Maria J. Silva, Artur M. S. Fernandes, Pedro A. Fernandes, Eduarda J Enzyme Inhib Med Chem Article α-Amylase has been considered an important therapeutic target for the management of type 2 diabetes mellitus (T2DM), decreasing postprandial hyperglycaemia (PPHG). In the present work, a panel of 40 structurally related flavonoids was tested, concerning their ability to inhibit α-amylase activity, using a microanalysis screening system, an inhibitory kinetic analysis and molecular docking calculations. From the obtained results, it was possible to observe that the flavone with a -Cl ion at 3-position of C-ring, an –OH group at 3′- and 4′- positions of B-ring and at 5- and 7- positions of A-ring and the C2 = C3 double bond, was the most active tested flavonoid, through competitive inhibition. In conclusion, some of the tested flavonoids have shown promising inhibition of α-amylase and may be considered as possible alternatives to the modulation of T2DM. Taylor & Francis 2019-02-06 /pmc/articles/PMC6366418/ /pubmed/30724629 http://dx.doi.org/10.1080/14756366.2018.1558221 Text en © 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. http://creativecommons.org/licenses/by/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Article
Proença, Carina
Freitas, Marisa
Ribeiro, Daniela
Tomé, Sara M.
Oliveira, Eduardo F. T.
Viegas, Matilde F.
Araújo, Alberto N.
Ramos, Maria J.
Silva, Artur M. S.
Fernandes, Pedro A.
Fernandes, Eduarda
Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title_full Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title_fullStr Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title_full_unstemmed Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title_short Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
title_sort evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6366418/
https://www.ncbi.nlm.nih.gov/pubmed/30724629
http://dx.doi.org/10.1080/14756366.2018.1558221
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