Natural plant alkaloid (Emetine) inhibits HIV-1 replication by interfering with reverse transcriptase activity.
Autor(a) principal: | |
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Data de Publicação: | 2015 |
Outros Autores: | , , , , , |
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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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 |
dc.date.issued.fl_str_mv |
2015 |
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2023-11-25T03:25:31Z |
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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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