Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity
Autor(a) principal: | |
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Data de Publicação: | 2013 |
Outros Autores: | , , , , , , , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10198/7873 |
Resumo: | Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases. |
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Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activitySolid dispersionEncapsulationAChEKineticBioactiveBerberis vulgarisResearchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases.The authors are grateful to CNPq and CAPES (Finance Code 001) for the support. The authors are grateful to the Foundation for Science and Technology (FCT, Portugal) for financial support through national funds FCT/MCTES to CIMO (UIDB/00690/2020). The authors are also grateful to FCT for financial support through national funds FCT/MCTES (PIDDAC) to CIMO (UIDB/00690/2020 and UIDP/00690/2020) and SusTEC (LA/P/0007/2020). L. Barros and C. Pereira thank FCT, P.I., for the contracts through the institutional scientific employment programcontract.ElsevierBiblioteca Digital do IPBLeimann, Fernanda VitóriaSouza, Luma Borges deOliveira, Byanca Pereira Moreira deRossi, Bruna FranzonSilva, Patricia Sabino daShiraishi, Carlos Seiti HurtadoKaplum, VanessaAbreu, Rui M.V.Pereira, CarlaBarros, LillianPeron, Ana PaulaIneu, Rafael PortoOechsler, Bruno FranciscoSayer, ClaudiaAraujo, Pedro Henrique Hermes deGonçalves, Odinei Hess2013-01-09T11:12:46Z20232023-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10198/7873engLeimann, Fernanda Vitória; Souza, Luma Borges de; Oliveira, Byanca Pereira Moreira de; Rossi, Bruna Franzon; Silva, Patricia Sabino da; Shiraishi, Carlos Seiti Hurtado; Kaplum, Vanessa; Abreu, Rui M.V.; Pereira, Carla; Barros, Lillian; Peron, Ana Paula; Ineu, Rafael Porto; Oechsler, Bruno Francisco; Sayer, Claudia: Araujo, Pedro Henrique Hermes de: Gonçalves, Odinei Hess (2023). Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity. Food Research International. eISSN 1873-7145. 173, p. 1-140963-996910.1016/j.foodres.2023.1132951873-7145info:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2023-12-06T01:17:24Zoai:bibliotecadigital.ipb.pt:10198/7873Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T00:41:18.265503Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse |
dc.title.none.fl_str_mv |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
title |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
spellingShingle |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity Leimann, Fernanda Vitória Solid dispersion Encapsulation AChE Kinetic Bioactive Berberis vulgaris |
title_short |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
title_full |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
title_fullStr |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
title_full_unstemmed |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
title_sort |
Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity |
author |
Leimann, Fernanda Vitória |
author_facet |
Leimann, Fernanda Vitória Souza, Luma Borges de Oliveira, Byanca Pereira Moreira de Rossi, Bruna Franzon Silva, Patricia Sabino da Shiraishi, Carlos Seiti Hurtado Kaplum, Vanessa Abreu, Rui M.V. Pereira, Carla Barros, Lillian Peron, Ana Paula Ineu, Rafael Porto Oechsler, Bruno Francisco Sayer, Claudia Araujo, Pedro Henrique Hermes de Gonçalves, Odinei Hess |
author_role |
author |
author2 |
Souza, Luma Borges de Oliveira, Byanca Pereira Moreira de Rossi, Bruna Franzon Silva, Patricia Sabino da Shiraishi, Carlos Seiti Hurtado Kaplum, Vanessa Abreu, Rui M.V. Pereira, Carla Barros, Lillian Peron, Ana Paula Ineu, Rafael Porto Oechsler, Bruno Francisco Sayer, Claudia Araujo, Pedro Henrique Hermes de Gonçalves, Odinei Hess |
author2_role |
author author author author author author author author author author author author author author author |
dc.contributor.none.fl_str_mv |
Biblioteca Digital do IPB |
dc.contributor.author.fl_str_mv |
Leimann, Fernanda Vitória Souza, Luma Borges de Oliveira, Byanca Pereira Moreira de Rossi, Bruna Franzon Silva, Patricia Sabino da Shiraishi, Carlos Seiti Hurtado Kaplum, Vanessa Abreu, Rui M.V. Pereira, Carla Barros, Lillian Peron, Ana Paula Ineu, Rafael Porto Oechsler, Bruno Francisco Sayer, Claudia Araujo, Pedro Henrique Hermes de Gonçalves, Odinei Hess |
dc.subject.por.fl_str_mv |
Solid dispersion Encapsulation AChE Kinetic Bioactive Berberis vulgaris |
topic |
Solid dispersion Encapsulation AChE Kinetic Bioactive Berberis vulgaris |
description |
Researchers have concentrated efforts in the search for natural-based reversible inhibitors for cholinesterase enzymes as they may play a key role in the treatment of degenerative diseases. Diverse plant alkaloids can inhibit the action of acetylcholinesterase and, among them, berberine is a promising bioactive. However, berberine has poor water solubility and low bioavailability, which makes it difficult to use in treatment. The solid dispersion technique can improve the water affinity of hydrophobic substances, but berberine solid dispersions have not been extensively studied. Safety testing is also essential to ensure that the berberine-loaded solid dispersions are safe for use. This study investigated the effectiveness of berberine-loaded solid dispersions (SD) as inhibitors of acetylcholinesterase enzyme (AChE). Docking simulation was used to investigate the influence of berberine on AChE, and in vitro assays were conducted to confirm the enzymatic kinetics of AChE in the presence of berberine. Berberine SD also showed improved cytotoxic effects on tumoral cells when dispersed in aqueous media. In vivo assays using Allium cepa were implemented, and no cytotoxicity/genotoxicity was found for the berberine solid dispersion. These results suggest that berberine SD could be a significant step towards safe nanostructures for use in the treatment of neurodegenerative diseases. |
publishDate |
2013 |
dc.date.none.fl_str_mv |
2013-01-09T11:12:46Z 2023 2023-01-01T00:00:00Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10198/7873 |
url |
http://hdl.handle.net/10198/7873 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
Leimann, Fernanda Vitória; Souza, Luma Borges de; Oliveira, Byanca Pereira Moreira de; Rossi, Bruna Franzon; Silva, Patricia Sabino da; Shiraishi, Carlos Seiti Hurtado; Kaplum, Vanessa; Abreu, Rui M.V.; Pereira, Carla; Barros, Lillian; Peron, Ana Paula; Ineu, Rafael Porto; Oechsler, Bruno Francisco; Sayer, Claudia: Araujo, Pedro Henrique Hermes de: Gonçalves, Odinei Hess (2023). Evaluation of berberine nanoparticles as a strategy to modulate acetylcholinesterase activity. Food Research International. eISSN 1873-7145. 173, p. 1-14 0963-9969 10.1016/j.foodres.2023.113295 1873-7145 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Elsevier |
publisher.none.fl_str_mv |
Elsevier |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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