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Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways

Twenty-eight neoflavonoids have been prepared and evaluated in vitro against HIV-1. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase reporter gene. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LT...

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Autores principales: Olmedo, Dionisio A., López-Pérez, José Luis, del Olmo, Esther, Bedoya, Luis M., Sancho, Rocío, Alcamí, José, Muñoz, Eduardo, San Feliciano, Arturo, Gupta, Mahabir P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155902/
https://www.ncbi.nlm.nih.gov/pubmed/28218730
http://dx.doi.org/10.3390/molecules22020321
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author Olmedo, Dionisio A.
López-Pérez, José Luis
del Olmo, Esther
Bedoya, Luis M.
Sancho, Rocío
Alcamí, José
Muñoz, Eduardo
San Feliciano, Arturo
Gupta, Mahabir P.
author_facet Olmedo, Dionisio A.
López-Pérez, José Luis
del Olmo, Esther
Bedoya, Luis M.
Sancho, Rocío
Alcamí, José
Muñoz, Eduardo
San Feliciano, Arturo
Gupta, Mahabir P.
author_sort Olmedo, Dionisio A.
collection PubMed
description Twenty-eight neoflavonoids have been prepared and evaluated in vitro against HIV-1. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase reporter gene. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Seven 4-phenylchromen-2-one derivatives showed HIV transcriptional inhibitory activity but only the phenylchrome-2-one 10 inhibited NF-κB and displayed anti-Tat activity simultaneously. Compounds 10, 14, and 25, inhibited HIV replication in both targets at concentrations <25 μM. The assays of these synthetic 4-phenylchromen-2-ones may aid in the investigation of some aspects of the anti-HIV activity of such compounds and could serve as a scaffold for designing better anti-HIV compounds, which may lead to a potential anti-HIV therapeutic drug.
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spelling pubmed-61559022018-11-13 Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways Olmedo, Dionisio A. López-Pérez, José Luis del Olmo, Esther Bedoya, Luis M. Sancho, Rocío Alcamí, José Muñoz, Eduardo San Feliciano, Arturo Gupta, Mahabir P. Molecules Article Twenty-eight neoflavonoids have been prepared and evaluated in vitro against HIV-1. Antiviral activity was assessed on MT-2 cells infected with viral clones carrying the luciferase reporter gene. Inhibition of HIV transcription and Tat function were tested on cells stably transfected with the HIV-LTR and Tat protein. Seven 4-phenylchromen-2-one derivatives showed HIV transcriptional inhibitory activity but only the phenylchrome-2-one 10 inhibited NF-κB and displayed anti-Tat activity simultaneously. Compounds 10, 14, and 25, inhibited HIV replication in both targets at concentrations <25 μM. The assays of these synthetic 4-phenylchromen-2-ones may aid in the investigation of some aspects of the anti-HIV activity of such compounds and could serve as a scaffold for designing better anti-HIV compounds, which may lead to a potential anti-HIV therapeutic drug. MDPI 2017-02-19 /pmc/articles/PMC6155902/ /pubmed/28218730 http://dx.doi.org/10.3390/molecules22020321 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Olmedo, Dionisio A.
López-Pérez, José Luis
del Olmo, Esther
Bedoya, Luis M.
Sancho, Rocío
Alcamí, José
Muñoz, Eduardo
San Feliciano, Arturo
Gupta, Mahabir P.
Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title_full Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title_fullStr Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title_full_unstemmed Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title_short Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
title_sort neoflavonoids as inhibitors of hiv-1 replication by targeting the tat and nf-κb pathways
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155902/
https://www.ncbi.nlm.nih.gov/pubmed/28218730
http://dx.doi.org/10.3390/molecules22020321
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