Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.

Detalhes bibliográficos
Autor(a) principal: Valadão, Ana Luiza Chaves
Data de Publicação: 2015
Outros Autores: Abreu, Celina Monteiro, Dias, Juliana Zanatta, Arantes, Pablo Ricardo, Verli, Hugo, Tanuri, Amilcar, Aguiar, Renato Santana
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UFRGS
Texto Completo: http://hdl.handle.net/10183/267592
Resumo: Ipecac alkaloids are secondary metabolites produced in the medicinal plant Psychotria ipecacuanha. Emetine is the main alkaloid of ipecac and one of the active compounds in syrup of Ipecac with emetic property. Here we evaluated emetine’s potential as an antiviral agent against Human Immunodeficiency Virus. We performed in vitro Reverse Transcriptase (RT) Assay and Natural Endogenous Reverse Transcriptase Activity Assay (NERT) to evaluate HIV RT inhibition. Emetine molecular docking on HIV-1 RT was also analyzed. Phenotypic assays were performed in non-lymphocytic and in Peripheral Blood Mononuclear Cells (PBMC) with HIV-1 wild-type and HIV-harboring RT-resistant mutation to Nucleoside Reverse Transcriptase Inhibitors (M184V). Our results showed that HIV-1 RT was blocked in the presence of emetine in both models: in vitro reactions with isolated HIV-1 RT and intravirion, measured by NERT. Emetine revealed a strong potential of inhibiting HIV-1 replication in both cellular models, reaching 80% of reduction in HIV-1 infection, with low cytotoxic effect. Emetine also blocked HIV-1 infection of RT M184V mutant. These results suggest that emetine is able to penetrate in intact HIV particles, and bind and block reverse transcription reaction, suggesting that it can be used as anti-HIV microbicide. Taken together, our findings provide additional pharmacological information on the potential therapeutic effects of emetine.
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spelling Valadão, Ana Luiza ChavesAbreu, Celina MonteiroDias, Juliana ZanattaArantes, Pablo RicardoVerli, HugoTanuri, AmilcarAguiar, Renato Santana2023-11-25T03:25:31Z20151420-3049http://hdl.handle.net/10183/267592000990962Ipecac alkaloids are secondary metabolites produced in the medicinal plant Psychotria ipecacuanha. Emetine is the main alkaloid of ipecac and one of the active compounds in syrup of Ipecac with emetic property. Here we evaluated emetine’s potential as an antiviral agent against Human Immunodeficiency Virus. We performed in vitro Reverse Transcriptase (RT) Assay and Natural Endogenous Reverse Transcriptase Activity Assay (NERT) to evaluate HIV RT inhibition. Emetine molecular docking on HIV-1 RT was also analyzed. Phenotypic assays were performed in non-lymphocytic and in Peripheral Blood Mononuclear Cells (PBMC) with HIV-1 wild-type and HIV-harboring RT-resistant mutation to Nucleoside Reverse Transcriptase Inhibitors (M184V). Our results showed that HIV-1 RT was blocked in the presence of emetine in both models: in vitro reactions with isolated HIV-1 RT and intravirion, measured by NERT. Emetine revealed a strong potential of inhibiting HIV-1 replication in both cellular models, reaching 80% of reduction in HIV-1 infection, with low cytotoxic effect. Emetine also blocked HIV-1 infection of RT M184V mutant. These results suggest that emetine is able to penetrate in intact HIV particles, and bind and block reverse transcription reaction, suggesting that it can be used as anti-HIV microbicide. Taken together, our findings provide additional pharmacological information on the potential therapeutic effects of emetine.application/pdfengMolecules. Basel, SW. Vol. 20, no. 4 (2015), p. 11474-11489HIV-1Transcriptase reversa do HIVEmetineReverse transcriptaseResistanceNatural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.Estrangeiroinfo:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFRGSinstname:Universidade Federal do Rio Grande do Sul (UFRGS)instacron:UFRGSTEXT000990962.pdf.txt000990962.pdf.txtExtracted Texttext/plain45008http://www.lume.ufrgs.br/bitstream/10183/267592/2/000990962.pdf.txtea90408b56a13f2cc30c83109cd52cb5MD52ORIGINAL000990962.pdfTexto completo (inglês)application/pdf1167920http://www.lume.ufrgs.br/bitstream/10183/267592/1/000990962.pdfae11484c4ebf4f6d59969fefe8cf3829MD5110183/2675922023-12-06 04:24:14.134671oai:www.lume.ufrgs.br:10183/267592Repositório de PublicaçõesPUBhttps://lume.ufrgs.br/oai/requestopendoar:2023-12-06T06:24:14Repositório Institucional da UFRGS - Universidade Federal do Rio Grande do Sul (UFRGS)false
dc.title.pt_BR.fl_str_mv Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
title Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
spellingShingle Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
Valadão, Ana Luiza Chaves
HIV-1
Transcriptase reversa do HIV
Emetine
Reverse transcriptase
Resistance
title_short Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
title_full Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
title_fullStr Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
title_full_unstemmed Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
title_sort Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
author Valadão, Ana Luiza Chaves
author_facet Valadão, Ana Luiza Chaves
Abreu, Celina Monteiro
Dias, Juliana Zanatta
Arantes, Pablo Ricardo
Verli, Hugo
Tanuri, Amilcar
Aguiar, Renato Santana
author_role author
author2 Abreu, Celina Monteiro
Dias, Juliana Zanatta
Arantes, Pablo Ricardo
Verli, Hugo
Tanuri, Amilcar
Aguiar, Renato Santana
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Valadão, Ana Luiza Chaves
Abreu, Celina Monteiro
Dias, Juliana Zanatta
Arantes, Pablo Ricardo
Verli, Hugo
Tanuri, Amilcar
Aguiar, Renato Santana
dc.subject.por.fl_str_mv HIV-1
Transcriptase reversa do HIV
topic HIV-1
Transcriptase reversa do HIV
Emetine
Reverse transcriptase
Resistance
dc.subject.eng.fl_str_mv Emetine
Reverse transcriptase
Resistance
description Ipecac alkaloids are secondary metabolites produced in the medicinal plant Psychotria ipecacuanha. Emetine is the main alkaloid of ipecac and one of the active compounds in syrup of Ipecac with emetic property. Here we evaluated emetine’s potential as an antiviral agent against Human Immunodeficiency Virus. We performed in vitro Reverse Transcriptase (RT) Assay and Natural Endogenous Reverse Transcriptase Activity Assay (NERT) to evaluate HIV RT inhibition. Emetine molecular docking on HIV-1 RT was also analyzed. Phenotypic assays were performed in non-lymphocytic and in Peripheral Blood Mononuclear Cells (PBMC) with HIV-1 wild-type and HIV-harboring RT-resistant mutation to Nucleoside Reverse Transcriptase Inhibitors (M184V). Our results showed that HIV-1 RT was blocked in the presence of emetine in both models: in vitro reactions with isolated HIV-1 RT and intravirion, measured by NERT. Emetine revealed a strong potential of inhibiting HIV-1 replication in both cellular models, reaching 80% of reduction in HIV-1 infection, with low cytotoxic effect. Emetine also blocked HIV-1 infection of RT M184V mutant. These results suggest that emetine is able to penetrate in intact HIV particles, and bind and block reverse transcription reaction, suggesting that it can be used as anti-HIV microbicide. Taken together, our findings provide additional pharmacological information on the potential therapeutic effects of emetine.
publishDate 2015
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dc.relation.ispartof.pt_BR.fl_str_mv Molecules. Basel, SW. Vol. 20, no. 4 (2015), p. 11474-11489
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