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Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition

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Resumo:A practical approach to control glycemia in diabetes is to use plant natural products that delay hydrolysis of complex sugars and promote the diminution of the release of glucosyl units into the blood plasma. Polyphenolics have been described as being effective in inhibiting amylases and α-glucosidases. Grape pomace is an important sub product of the wine industry, still rich in many compounds such as polyphenolics. In this context, the purpose of this study was to search for possible effects of a grape pomace extract on salivary and pancreatic α-amylases and α-glucosidase, as well as on intestinal glucose absorption. The Merlot grape pomace extract (MGPE) was prepared using a hydroalcoholic mixture (40% ethanol + 60% water). In vitro inhibition was quantified using potato starch (for amylases) and maltose (for α-glucosidase) as substrates. In vivo inhibition was evaluated by running starch and maltose tolerance tests in rats with or without administration of MGPE. Ranking of the extract compounds for its affinity to the α-amylases was accomplished by computer simulations using three different programs. Both α-amylases, pancreatic and salivary, were inhibited by the MGPE. No inhibition on α-glucosidase, however, was detected. The IC50 values were 90 ± 10 μg/mL and 143 ± 15 μg/mL for salivary and pancreatic amylases, respectively. Kinetically this inhibition showed a complex pattern, with multiple binding of the extract constituents to the enzymes. Furthermore, the in silico docking simulations indicated that several phenolic substances, e.g., peonidin-3-O-acetylglucoside, quercetin-3-O-glucuronide and isorhamnetin-3-O-glucoside, besides catechin, were the most likely polyphenols responsible for the α-amylase inhibition caused by MGPE. The hyperglycemic burst, an usual phenomenon that follows starch administration, was substantially inhibited by the MGPE. Our results suggest that the MGPE can be adequate for maintaining normal blood levels after food ingestion.
Autores principais:Kato-Schwartz, Camila Gabriel
Outros Autores:Corrêa, Rúbia C.G.; Lima, Diego de Souza; Sá-Nakanishi, Anacharis B. de; Gonçalves, Geferson A.; Seixas, Flávio Augusto Vicente; Haminiuk, Charles Windson Isidoro; Barros, Lillian; Ferreira, Isabel C.F.R.; Bracht, Adelar; Peralta, Rosane M.
Assunto:Carbohydrate-hydrolysing enzymes Diabetes Docking simulations Flavonoids Glycemia control Polyphenols Winery by-product
Ano:2020
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso aberto
Instituição associada:Instituto Politécnico de Bragança
Idioma:inglês
Origem:Biblioteca Digital do IPB
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author Kato-Schwartz, Camila Gabriel
author2 Corrêa, Rúbia C.G.
Lima, Diego de Souza
Sá-Nakanishi, Anacharis B. de
Gonçalves, Geferson A.
Seixas, Flávio Augusto Vicente
Haminiuk, Charles Windson Isidoro
Barros, Lillian
Ferreira, Isabel C.F.R.
Bracht, Adelar
Peralta, Rosane M.
author2_role author
author
author
author
author
author
author
author
author
author
author_facet Kato-Schwartz, Camila Gabriel
Corrêa, Rúbia C.G.
Lima, Diego de Souza
Sá-Nakanishi, Anacharis B. de
Gonçalves, Geferson A.
Seixas, Flávio Augusto Vicente
Haminiuk, Charles Windson Isidoro
Barros, Lillian
Ferreira, Isabel C.F.R.
Bracht, Adelar
Peralta, Rosane M.
author_role author
contributor_name_str_mv Biblioteca Digital do IPB
country_str PT
creators_json_txt [{\"Person.name\":\"Kato-Schwartz, Camila Gabriel\"},{\"Person.name\":\"Corrêa, Rúbia C.G.\",\"Person.identifier.orcid\":\"0000-0003-0269-4344\"},{\"Person.name\":\"Lima, Diego de Souza\"},{\"Person.name\":\"Sá-Nakanishi, Anacharis B. de\"},{\"Person.name\":\"Gonçalves, Geferson A.\"},{\"Person.name\":\"Seixas, Flávio Augusto Vicente\"},{\"Person.name\":\"Haminiuk, Charles Windson Isidoro\"},{\"Person.name\":\"Barros, Lillian\",\"Person.identifier.orcid\":\"0000-0002-9050-5189\"},{\"Person.name\":\"Ferreira, Isabel C.F.R.\",\"Person.identifier.orcid\":\"0000-0003-4910-4882\"},{\"Person.name\":\"Bracht, Adelar\"},{\"Person.name\":\"Peralta, Rosane M.\"}]
datacite.contributors.contributor.contributorName.fl_str_mv Biblioteca Digital do IPB
datacite.creators.creator.creatorName.fl_str_mv Kato-Schwartz, Camila Gabriel
Corrêa, Rúbia C.G.
Lima, Diego de Souza
Sá-Nakanishi, Anacharis B. de
Gonçalves, Geferson A.
Seixas, Flávio Augusto Vicente
Haminiuk, Charles Windson Isidoro
Barros, Lillian
Ferreira, Isabel C.F.R.
Bracht, Adelar
Peralta, Rosane M.
datacite.date.Accepted.fl_str_mv 2020-01-01T00:00:00Z
datacite.date.available.fl_str_mv 2018-01-19T10:00:00Z
datacite.date.embargoed.fl_str_mv 2018-01-19T10:00:00Z
datacite.rights.fl_str_mv http://purl.org/coar/access_right/c_abf2
datacite.subjects.subject.fl_str_mv Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
datacite.titles.title.fl_str_mv Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
dc.contributor.none.fl_str_mv Biblioteca Digital do IPB
dc.creator.none.fl_str_mv Kato-Schwartz, Camila Gabriel
Corrêa, Rúbia C.G.
Lima, Diego de Souza
Sá-Nakanishi, Anacharis B. de
Gonçalves, Geferson A.
Seixas, Flávio Augusto Vicente
Haminiuk, Charles Windson Isidoro
Barros, Lillian
Ferreira, Isabel C.F.R.
Bracht, Adelar
Peralta, Rosane M.
dc.date.Accepted.fl_str_mv 2020-01-01T00:00:00Z
dc.date.available.fl_str_mv 2018-01-19T10:00:00Z
dc.date.embargoed.fl_str_mv 2018-01-19T10:00:00Z
dc.format.none.fl_str_mv application/pdf
dc.identifier.none.fl_str_mv http://hdl.handle.net/10198/23365
dc.language.none.fl_str_mv eng
dc.rights.none.fl_str_mv http://purl.org/coar/access_right/c_abf2
dc.subject.none.fl_str_mv Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
dc.title.fl_str_mv Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
dc.type.none.fl_str_mv http://purl.org/coar/resource_type/c_6501
description A practical approach to control glycemia in diabetes is to use plant natural products that delay hydrolysis of complex sugars and promote the diminution of the release of glucosyl units into the blood plasma. Polyphenolics have been described as being effective in inhibiting amylases and α-glucosidases. Grape pomace is an important sub product of the wine industry, still rich in many compounds such as polyphenolics. In this context, the purpose of this study was to search for possible effects of a grape pomace extract on salivary and pancreatic α-amylases and α-glucosidase, as well as on intestinal glucose absorption. The Merlot grape pomace extract (MGPE) was prepared using a hydroalcoholic mixture (40% ethanol + 60% water). In vitro inhibition was quantified using potato starch (for amylases) and maltose (for α-glucosidase) as substrates. In vivo inhibition was evaluated by running starch and maltose tolerance tests in rats with or without administration of MGPE. Ranking of the extract compounds for its affinity to the α-amylases was accomplished by computer simulations using three different programs. Both α-amylases, pancreatic and salivary, were inhibited by the MGPE. No inhibition on α-glucosidase, however, was detected. The IC50 values were 90 ± 10 μg/mL and 143 ± 15 μg/mL for salivary and pancreatic amylases, respectively. Kinetically this inhibition showed a complex pattern, with multiple binding of the extract constituents to the enzymes. Furthermore, the in silico docking simulations indicated that several phenolic substances, e.g., peonidin-3-O-acetylglucoside, quercetin-3-O-glucuronide and isorhamnetin-3-O-glucoside, besides catechin, were the most likely polyphenols responsible for the α-amylase inhibition caused by MGPE. The hyperglycemic burst, an usual phenomenon that follows starch administration, was substantially inhibited by the MGPE. Our results suggest that the MGPE can be adequate for maintaining normal blood levels after food ingestion.
dirty 0
eu_rights_str_mv openAccess
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identifier.url.fl_str_mv http://hdl.handle.net/10198/23365
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instname_str Instituto Politécnico de Bragança
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oai_identifier_str oai:bibliotecadigital.ipb.pt:10198/23365
organization_str_mv urn:organizationAcronym:ipb
person_str_mv Kato-Schwartz, Camila Gabriel
Corrêa, Rúbia C.G.
Corrêa, Rúbia C.G.
https://www.ciencia-id.pt/6C1F-2818-CBB5
6C1F-2818-CBB5
http://orcid.org/0000-0003-0269-4344
0000-0003-0269-4344
Lima, Diego de Souza
Sá-Nakanishi, Anacharis B. de
Gonçalves, Geferson A.
Seixas, Flávio Augusto Vicente
Haminiuk, Charles Windson Isidoro
Barros, Lillian
Barros, Lillian
https://www.ciencia-id.pt/9616-35CB-D001
9616-35CB-D001
http://orcid.org/0000-0002-9050-5189
0000-0002-9050-5189
Ferreira, Isabel C.F.R.
Ferreira, Isabel C.F.R.
https://www.ciencia-id.pt/9418-CF95-9919
9418-CF95-9919
http://orcid.org/0000-0003-4910-4882
0000-0003-4910-4882
Bracht, Adelar
Peralta, Rosane M.
publishDate 2020
reponame_str Biblioteca Digital do IPB
repository_id_str urn:repositoryAcronym:ipb
service_str_mv urn:repositoryAcronym:ipb
spelling engen_ENA practical approach to control glycemia in diabetes is to use plant natural products that delay hydrolysis of complex sugars and promote the diminution of the release of glucosyl units into the blood plasma. Polyphenolics have been described as being effective in inhibiting amylases and α-glucosidases. Grape pomace is an important sub product of the wine industry, still rich in many compounds such as polyphenolics. In this context, the purpose of this study was to search for possible effects of a grape pomace extract on salivary and pancreatic α-amylases and α-glucosidase, as well as on intestinal glucose absorption. The Merlot grape pomace extract (MGPE) was prepared using a hydroalcoholic mixture (40% ethanol + 60% water). In vitro inhibition was quantified using potato starch (for amylases) and maltose (for α-glucosidase) as substrates. In vivo inhibition was evaluated by running starch and maltose tolerance tests in rats with or without administration of MGPE. Ranking of the extract compounds for its affinity to the α-amylases was accomplished by computer simulations using three different programs. Both α-amylases, pancreatic and salivary, were inhibited by the MGPE. No inhibition on α-glucosidase, however, was detected. The IC50 values were 90 ± 10 μg/mL and 143 ± 15 μg/mL for salivary and pancreatic amylases, respectively. Kinetically this inhibition showed a complex pattern, with multiple binding of the extract constituents to the enzymes. Furthermore, the in silico docking simulations indicated that several phenolic substances, e.g., peonidin-3-O-acetylglucoside, quercetin-3-O-glucuronide and isorhamnetin-3-O-glucoside, besides catechin, were the most likely polyphenols responsible for the α-amylase inhibition caused by MGPE. The hyperglycemic burst, an usual phenomenon that follows starch administration, was substantially inhibited by the MGPE. Our results suggest that the MGPE can be adequate for maintaining normal blood levels after food ingestion.application/pdfen_ENPotential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibitionKato-Schwartz, Camila GabrielPersonalCorrêa, Rúbia C.G.DSpacehttp://dspace.org/items/35cf5f0f-d5bc-49ad-9704-e6613e60f0fcDSpacehttp://dspace.org/items/35cf5f0f-d5bc-49ad-9704-e6613e60f0fcCorrêaRúbia C.G.Ciência IDhttps://www.ciencia-id.pt6C1F-2818-CBB5ORCIDhttp://orcid.org0000-0003-0269-4344Scopus Author IDhttps://www.scopus.com37661286600Lima, Diego de SouzaSá-Nakanishi, Anacharis B. deGonçalves, Geferson A.Seixas, Flávio Augusto VicenteHaminiuk, Charles Windson IsidoroPersonalBarros, LillianDSpacehttp://dspace.org/items/3af07ffe-f914-48ba-a5d5-efcf70fdce01DSpacehttp://dspace.org/items/3af07ffe-f914-48ba-a5d5-efcf70fdce01BarrosLillianCiência IDhttps://www.ciencia-id.pt9616-35CB-D001ORCIDhttp://orcid.org0000-0002-9050-5189Researcher IDhttps://www.researcherid.comJ-3600-2013Researcher IDhttps://www.researcherid.comJ-3600-2013Scopus Author IDhttps://www.scopus.com35236343600Scopus Author IDhttps://www.scopus.com57194900801PersonalFerreira, Isabel C.F.R.DSpacehttp://dspace.org/items/bd0d1537-2e03-41fb-b27a-140af9c35db8DSpacehttp://dspace.org/items/bd0d1537-2e03-41fb-b27a-140af9c35db8FerreiraIsabel C.F.R.Ciência IDhttps://www.ciencia-id.pt9418-CF95-9919ORCIDhttp://orcid.org0000-0003-4910-4882Researcher IDhttps://www.researcherid.comE-8500-2013Scopus Author IDhttps://www.scopus.com36868826600Bracht, AdelarPeralta, Rosane M.HostingInstitutionOrganizationalBiblioteca Digital do IPBe-mailmailto:dspace@ipb.ptdspace@ipb.ptISSNIsPartOf0963-9969DOIIsPartOf10.1016/j.foodres.2020.1094622018-01-19T10:00:00Z20202020-01-01T00:00:00ZHandlehttp://hdl.handle.net/10198/23365http://purl.org/coar/access_right/c_abf2open accessCarbohydrate-hydrolysing enzymesDiabetesDocking simulationsFlavonoidsGlycemia controlPolyphenolsWinery by-product611482 bytesliteraturehttp://purl.org/coar/resource_type/c_6501journal articlehttp://purl.org/coar/access_right/c_abf2application/pdffulltexthttps://bibliotecadigital.ipb.pt/bitstreams/0f1a9db7-59b2-4b89-a6ee-697ef4719ae5/download
spellingShingle Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
Kato-Schwartz, Camila Gabriel
Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
status SINGLETON
subject.fl_str_mv Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
title Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
title_full Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
title_fullStr Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
title_full_unstemmed Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
title_short Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
title_sort Potential anti-diabetic properties of Merlot grape pomace extract: an in vitro, in silico and in vivo study of α-amylase and α-glucosidase inhibition
topic Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
topic_facet Carbohydrate-hydrolysing enzymes
Diabetes
Docking simulations
Flavonoids
Glycemia control
Polyphenols
Winery by-product
url http://hdl.handle.net/10198/23365
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