In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium

Detalhes bibliográficos
Autor(a) principal: Arcanjo, Daniel D. R.
Data de Publicação: 2016
Outros Autores: Mafud, Ana Carolina, Vasconcelos, Andreanne G., Silva-Filho, José Couras da, Amaral, Maurício P. M., Brito, Lucas M., Bemquerer, Marcelo P., Kückelhaus, Selma A. S., Plácido, Alexandra, Delerue-Matos, Cristina, Vale, Nuno, Mascarenhas, Yvonne P., Carvalho, Fernando Aécio A., Oliveira, Aldeidia P., Leite, José Roberto Souza Almeida
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10400.22/13629
Resumo: BPP-BrachyNH2 is a proline-rich oligopeptide (PRO) firstly identified in skin secretion of the frog Brachycephalus ephippium, which possess in vitro inhibitory activity of angiotensin-I converting enzyme (ACE) and endothelium-dependent vasorelaxant activity. Considering its potential application in the treatment of cardiovascular diseases, the present work assessed the toxicological profile of the BPP-BrachyNH2. The in silico toxicity prediction was performed from the best model obtained through the optimization of the FASTA query peptide. This prediction study revealed that BPP-BrachyNH2 induced high predicted LD50 values for both humans and rats, and then is well-tolerated in the recommended range. The MTT assay was applied for the in vitro cytotoxic evaluation in murine macrophages. In this assay, a decrease of cell viability was not observed. The in vivo acute toxicological study was performed after the intraperitoneal administration of BPP-BrachyNH2 at doses of 5 and 50 mg/kg. After intraperitoneal administration, no death, alterations in behavioral parameters or weight gain curve was observed, as well as none in the serum biochemical parameters, and gross pathological and histopathological analyses. These observations demonstrates an acceptable safety profile for BPP-BrachyNH2, leading towards further studies focused on investigation of pharmacological and therapeutical applications for this peptide.
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spelling In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippiumCytotoxicityMTTIn silicopkCSMProline-rich oligopeptideToxicologicalBPP-BrachyNH2 is a proline-rich oligopeptide (PRO) firstly identified in skin secretion of the frog Brachycephalus ephippium, which possess in vitro inhibitory activity of angiotensin-I converting enzyme (ACE) and endothelium-dependent vasorelaxant activity. Considering its potential application in the treatment of cardiovascular diseases, the present work assessed the toxicological profile of the BPP-BrachyNH2. The in silico toxicity prediction was performed from the best model obtained through the optimization of the FASTA query peptide. This prediction study revealed that BPP-BrachyNH2 induced high predicted LD50 values for both humans and rats, and then is well-tolerated in the recommended range. The MTT assay was applied for the in vitro cytotoxic evaluation in murine macrophages. In this assay, a decrease of cell viability was not observed. The in vivo acute toxicological study was performed after the intraperitoneal administration of BPP-BrachyNH2 at doses of 5 and 50 mg/kg. After intraperitoneal administration, no death, alterations in behavioral parameters or weight gain curve was observed, as well as none in the serum biochemical parameters, and gross pathological and histopathological analyses. These observations demonstrates an acceptable safety profile for BPP-BrachyNH2, leading towards further studies focused on investigation of pharmacological and therapeutical applications for this peptide.Repositório Científico do Instituto Politécnico do PortoArcanjo, Daniel D. R.Mafud, Ana CarolinaVasconcelos, Andreanne G.Silva-Filho, José Couras daAmaral, Maurício P. M.Brito, Lucas M.Bemquerer, Marcelo P.Kückelhaus, Selma A. S.Plácido, AlexandraDelerue-Matos, CristinaVale, NunoMascarenhas, Yvonne P.Carvalho, Fernando Aécio A.Oliveira, Aldeidia P.Leite, José Roberto Souza Almeida2019-04-17T14:39:01Z20162016-01-01T00:00:00Zinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10400.22/13629eng1573-314910.1007/s10989-016-9564-2info: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:RCAAP2023-03-13T12:55:21Zoai:recipp.ipp.pt:10400.22/13629Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-19T17:33:29.034643Repositório 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 In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
title In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
spellingShingle In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
Arcanjo, Daniel D. R.
Cytotoxicity
MTT
In silico
pkCSM
Proline-rich oligopeptide
Toxicological
title_short In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
title_full In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
title_fullStr In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
title_full_unstemmed In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
title_sort In Silico, In Vitro and In Vivo Toxicological Assessment of BPP-BrachyNH2, A Vasoactive Proline-Rich Oligopeptide from Brachycephalus ephippium
author Arcanjo, Daniel D. R.
author_facet Arcanjo, Daniel D. R.
Mafud, Ana Carolina
Vasconcelos, Andreanne G.
Silva-Filho, José Couras da
Amaral, Maurício P. M.
Brito, Lucas M.
Bemquerer, Marcelo P.
Kückelhaus, Selma A. S.
Plácido, Alexandra
Delerue-Matos, Cristina
Vale, Nuno
Mascarenhas, Yvonne P.
Carvalho, Fernando Aécio A.
Oliveira, Aldeidia P.
Leite, José Roberto Souza Almeida
author_role author
author2 Mafud, Ana Carolina
Vasconcelos, Andreanne G.
Silva-Filho, José Couras da
Amaral, Maurício P. M.
Brito, Lucas M.
Bemquerer, Marcelo P.
Kückelhaus, Selma A. S.
Plácido, Alexandra
Delerue-Matos, Cristina
Vale, Nuno
Mascarenhas, Yvonne P.
Carvalho, Fernando Aécio A.
Oliveira, Aldeidia P.
Leite, José Roberto Souza Almeida
author2_role author
author
author
author
author
author
author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Repositório Científico do Instituto Politécnico do Porto
dc.contributor.author.fl_str_mv Arcanjo, Daniel D. R.
Mafud, Ana Carolina
Vasconcelos, Andreanne G.
Silva-Filho, José Couras da
Amaral, Maurício P. M.
Brito, Lucas M.
Bemquerer, Marcelo P.
Kückelhaus, Selma A. S.
Plácido, Alexandra
Delerue-Matos, Cristina
Vale, Nuno
Mascarenhas, Yvonne P.
Carvalho, Fernando Aécio A.
Oliveira, Aldeidia P.
Leite, José Roberto Souza Almeida
dc.subject.por.fl_str_mv Cytotoxicity
MTT
In silico
pkCSM
Proline-rich oligopeptide
Toxicological
topic Cytotoxicity
MTT
In silico
pkCSM
Proline-rich oligopeptide
Toxicological
description BPP-BrachyNH2 is a proline-rich oligopeptide (PRO) firstly identified in skin secretion of the frog Brachycephalus ephippium, which possess in vitro inhibitory activity of angiotensin-I converting enzyme (ACE) and endothelium-dependent vasorelaxant activity. Considering its potential application in the treatment of cardiovascular diseases, the present work assessed the toxicological profile of the BPP-BrachyNH2. The in silico toxicity prediction was performed from the best model obtained through the optimization of the FASTA query peptide. This prediction study revealed that BPP-BrachyNH2 induced high predicted LD50 values for both humans and rats, and then is well-tolerated in the recommended range. The MTT assay was applied for the in vitro cytotoxic evaluation in murine macrophages. In this assay, a decrease of cell viability was not observed. The in vivo acute toxicological study was performed after the intraperitoneal administration of BPP-BrachyNH2 at doses of 5 and 50 mg/kg. After intraperitoneal administration, no death, alterations in behavioral parameters or weight gain curve was observed, as well as none in the serum biochemical parameters, and gross pathological and histopathological analyses. These observations demonstrates an acceptable safety profile for BPP-BrachyNH2, leading towards further studies focused on investigation of pharmacological and therapeutical applications for this peptide.
publishDate 2016
dc.date.none.fl_str_mv 2016
2016-01-01T00:00:00Z
2019-04-17T14:39:01Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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dc.identifier.uri.fl_str_mv http://hdl.handle.net/10400.22/13629
url http://hdl.handle.net/10400.22/13629
dc.language.iso.fl_str_mv eng
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dc.relation.none.fl_str_mv 1573-3149
10.1007/s10989-016-9564-2
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