Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.

Detalhes bibliográficos
Autor(a) principal: Chierrito, Talita Perez Cantuaria
Data de Publicação: 2014
Outros Autores: Aguiar, Anna Caroline Campos, Andrade, Isabel Mayer de, Cerávolo, Isabela Penna, Gonçalves, Regina AC, Oliveira, Arildo JB de, Krettli, Antoniana Ursine
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da FIOCRUZ (ARCA)
Texto Completo: https://www.arca.fiocruz.br/handle/icict/9481
Resumo: Universidade Estadual de Maringá. Programa de Pós-Graduação em Ciências Farmacêuticas. Maringá, PR, Brazil
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spelling Chierrito, Talita Perez CantuariaAguiar, Anna Caroline CamposAndrade, Isabel Mayer deCerávolo, Isabela PennaGonçalves, Regina ACOliveira, Arildo JB deKrettli, Antoniana Ursine2015-02-10T18:13:54Z2015-02-10T18:13:54Z2014CHIERRITO, Talita Perez Cantuaria. Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum. Chierrito et al. Malaria Journal, v. 13, p. 142 2014.1475-2875https://www.arca.fiocruz.br/handle/icict/948110.1186/1475-2875-13-142engBioMed Central LtdAnti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleUniversidade Estadual de Maringá. Programa de Pós-Graduação em Ciências Farmacêuticas. Maringá, PR, BrazilUniversidade Federal de Minas Gerais. Programa de Pós-Graduação em Medicina Molecular. Belo Horizonte, MG, Brazil/Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária.Belo Horizonte, MG, BrazilFundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, BrazilUniversidade Estadual de Maringá. Programa de Pós-Graduação em Ciências Farmacêuticas. Maringá, PR, BrazilUniversidade Estadual de Maringá. Programa de Pós-Graduação em Ciências Farmacêuticas. Maringá, PR, BrazilUniversidade Federal de Minas Gerais. Programa de Pós-Graduação em Medicina Molecular. Belo Horizonte, MG, Brazil/Fundação Oswaldo Cruz. Centro de Pesquisas René Rachou. Laboratório de Malária. Belo Horizonte, MG, BrazilBackground: Several species of Aspidosperma (Apocynaceae) are used as treatments for human diseases in the tropics. Aspidosperma olivaceum, which is used to treat fevers in some regions of Brazil, contains the monoterpenoid indole alkaloids (MIAs) aspidoscarpine, uleine, apparicine, and N-methyl-tetrahydrolivacine. Using bio-guided fractionation and cytotoxicity testing in a human hepatoma cell line, several plant fractions and compounds purified from the bark and leaves of the plant were characterized for specific therapeutic activity (and selectivity index, SI) in vitro against the blood forms of Plasmodium falciparum. Methods: The activity of A. olivaceum extracts, fractions, and isolated compounds was evaluated against chloroquine (CQ)-resistant P. falciparum blood parasites by in vitro testing with radiolabelled [3H]-hypoxanthine and a monoclonal anti-histidine-rich protein (HRPII) antibody. The cytotoxicity of these fractions and compounds was evaluated in a human hepatoma cell line using a 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assay, and the SI was calculated as the ratio between the toxicity and activity. Two leaf fractions were tested in mice with Plasmodium berghei. Results: All six fractions from the bark and leaf extracts were active in vitro at low doses (IC50 < 5.0 μg/mL) using the anti-HRPII test, and only two (the neutral and basic bark fractions) were toxic to a human cell line (HepG2). The most promising fractions were the crude leaf extract and its basic residue, which had SIs above 50. Among the four pure compounds evaluated, aspidoscarpine in the bark and leaf extracts showed the highest SI at 56; this compound, therefore, represents a possible anti-malarial drug that requires further study. The acidic leaf fraction administered by gavage to mice with blood-induced malaria was also active. Conclusion: Using a bio-monitoring approach, it was possible to attribute the anti-P. falciparum activity of A. olivaceum to aspidoscarpine and, to a lesser extent, N-methyl-tetrahydrolivacine; other isolated MIA molecules were active but had lower SIs due to their higher toxicities. These results stood in contrast to previous work in which the anti-malarial activity of other Aspidosperma species was attributed to uleine.Aspidosperma olivaceumIndole alkaloidsAspidoscarpineMedicinal plantsAntimalarialPlasmodium falciparuminfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txtlicense.txttext/plain; charset=utf-81914https://www.arca.fiocruz.br/bitstream/icict/9481/1/license.txt7d48279ffeed55da8dfe2f8e81f3b81fMD51ORIGINAL2014_071.pdf2014_071.pdfapplication/pdf1238599https://www.arca.fiocruz.br/bitstream/icict/9481/2/2014_071.pdfc237ab822bf016f3cf9ad98a3f9a7759MD52TEXT2014_071.pdf.txt2014_071.pdf.txtExtracted texttext/plain40376https://www.arca.fiocruz.br/bitstream/icict/9481/3/2014_071.pdf.txtf66938c08602f54a4308e3052ad33b71MD53icict/94812019-06-19 10:07:37.462oai:www.arca.fiocruz.br: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ório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352019-06-19T13:07:37Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false
dc.title.pt_BR.fl_str_mv Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
title Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
spellingShingle Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
Chierrito, Talita Perez Cantuaria
Aspidosperma olivaceum
Indole alkaloids
Aspidoscarpine
Medicinal plants
Antimalarial
Plasmodium falciparum
title_short Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
title_full Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
title_fullStr Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
title_full_unstemmed Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
title_sort Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum.
author Chierrito, Talita Perez Cantuaria
author_facet Chierrito, Talita Perez Cantuaria
Aguiar, Anna Caroline Campos
Andrade, Isabel Mayer de
Cerávolo, Isabela Penna
Gonçalves, Regina AC
Oliveira, Arildo JB de
Krettli, Antoniana Ursine
author_role author
author2 Aguiar, Anna Caroline Campos
Andrade, Isabel Mayer de
Cerávolo, Isabela Penna
Gonçalves, Regina AC
Oliveira, Arildo JB de
Krettli, Antoniana Ursine
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Chierrito, Talita Perez Cantuaria
Aguiar, Anna Caroline Campos
Andrade, Isabel Mayer de
Cerávolo, Isabela Penna
Gonçalves, Regina AC
Oliveira, Arildo JB de
Krettli, Antoniana Ursine
dc.subject.en.pt_BR.fl_str_mv Aspidosperma olivaceum
Indole alkaloids
Aspidoscarpine
Medicinal plants
Antimalarial
Plasmodium falciparum
topic Aspidosperma olivaceum
Indole alkaloids
Aspidoscarpine
Medicinal plants
Antimalarial
Plasmodium falciparum
description Universidade Estadual de Maringá. Programa de Pós-Graduação em Ciências Farmacêuticas. Maringá, PR, Brazil
publishDate 2014
dc.date.issued.fl_str_mv 2014
dc.date.accessioned.fl_str_mv 2015-02-10T18:13:54Z
dc.date.available.fl_str_mv 2015-02-10T18:13:54Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
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status_str publishedVersion
dc.identifier.citation.fl_str_mv CHIERRITO, Talita Perez Cantuaria. Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum. Chierrito et al. Malaria Journal, v. 13, p. 142 2014.
dc.identifier.uri.fl_str_mv https://www.arca.fiocruz.br/handle/icict/9481
dc.identifier.issn.none.fl_str_mv 1475-2875
dc.identifier.doi.none.fl_str_mv 10.1186/1475-2875-13-142
identifier_str_mv CHIERRITO, Talita Perez Cantuaria. Anti-malarial activity of indole alkaloids isolated from Aspidosperma olivaceum. Chierrito et al. Malaria Journal, v. 13, p. 142 2014.
1475-2875
10.1186/1475-2875-13-142
url https://www.arca.fiocruz.br/handle/icict/9481
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dc.publisher.none.fl_str_mv BioMed Central Ltd
publisher.none.fl_str_mv BioMed Central Ltd
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