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...
| Autores: | , , , , , , , , |
|---|---|
| Tipo de recurso: | artículo |
| Fecha de publicación: | 2017 |
| País: | España |
| Institución: | Universidad Complutense de Madrid (UCM) |
| Repositorio: | Docta Complutense |
| Idioma: | inglés |
| OAI Identifier: | oai:docta.ucm.es:20.500.14352/19242 |
| Acceso en línea: | https://hdl.handle.net/20.500.14352/19242 |
| Access Level: | acceso abierto |
| Palabra clave: | 615.011 Neoflavonoids 4-phenyl-chromen-one AIDS Tat protein NF-κB inhibition Anti-HIV activity Farmacología (Farmacia) Química farmaceútica 3209 Farmacología 2390 Química Farmacéutica |
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Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB PathwaysOlmedo, Dionisio A.López-Pérez, José Luisdel Olmo, EstherBedoya Del Olmo, Luis MiguelSancho, RocíoAlcamí, JoséMuñoz, EduardoSan Feliciano, ArturoGupta, Mahabir P.615.011Neoflavonoids4-phenyl-chromen-oneAIDSTat proteinNF-κB inhibitionAnti-HIV activityFarmacología (Farmacia)Química farmaceútica3209 Farmacología2390 Química FarmacéuticaTwenty-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.MDPIUniversidad Complutense de Madrid20172017-02-1920172017-02-19journal articlehttp://purl.org/coar/resource_type/c_6501info:eu-repo/semantics/articleapplication/pdfhttps://hdl.handle.net/20.500.14352/19242reponame:Docta Complutenseinstname:Universidad Complutense de Madrid (UCM)Inglésengopen accesshttp://purl.org/coar/access_right/c_abf2Atribución 3.0 Españahttps://creativecommons.org/licenses/by/3.0/es/info:eu-repo/semantics/openAccessoai:docta.ucm.es:20.500.14352/192422026-06-02T12:44:21Z |
| dc.title.none.fl_str_mv |
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 |
| spellingShingle |
Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways Olmedo, Dionisio A. 615.011 Neoflavonoids 4-phenyl-chromen-one AIDS Tat protein NF-κB inhibition Anti-HIV activity Farmacología (Farmacia) Química farmaceútica 3209 Farmacología 2390 Química Farmacéutica |
| title_short |
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_sort |
Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways |
| dc.creator.none.fl_str_mv |
Olmedo, Dionisio A. López-Pérez, José Luis del Olmo, Esther Bedoya Del Olmo, Luis Miguel Sancho, Rocío Alcamí, José Muñoz, Eduardo San Feliciano, Arturo Gupta, Mahabir P. |
| author |
Olmedo, Dionisio A. |
| author_facet |
Olmedo, Dionisio A. López-Pérez, José Luis del Olmo, Esther Bedoya Del Olmo, Luis Miguel Sancho, Rocío Alcamí, José Muñoz, Eduardo San Feliciano, Arturo Gupta, Mahabir P. |
| author_role |
author |
| author2 |
López-Pérez, José Luis del Olmo, Esther Bedoya Del Olmo, Luis Miguel Sancho, Rocío Alcamí, José Muñoz, Eduardo San Feliciano, Arturo Gupta, Mahabir P. |
| author2_role |
author author author author author author author author |
| dc.contributor.none.fl_str_mv |
Universidad Complutense de Madrid |
| dc.subject.none.fl_str_mv |
615.011 Neoflavonoids 4-phenyl-chromen-one AIDS Tat protein NF-κB inhibition Anti-HIV activity Farmacología (Farmacia) Química farmaceútica 3209 Farmacología 2390 Química Farmacéutica |
| topic |
615.011 Neoflavonoids 4-phenyl-chromen-one AIDS Tat protein NF-κB inhibition Anti-HIV activity Farmacología (Farmacia) Química farmaceútica 3209 Farmacología 2390 Química Farmacéutica |
| 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. |
| publishDate |
2017 |
| dc.date.none.fl_str_mv |
2017 2017-02-19 2017 2017-02-19 |
| dc.type.none.fl_str_mv |
journal article http://purl.org/coar/resource_type/c_6501 |
| dc.type.openaire.fl_str_mv |
info:eu-repo/semantics/article |
| format |
article |
| dc.identifier.none.fl_str_mv |
https://hdl.handle.net/20.500.14352/19242 |
| url |
https://hdl.handle.net/20.500.14352/19242 |
| dc.language.none.fl_str_mv |
Inglés eng |
| language_invalid_str_mv |
Inglés |
| language |
eng |
| dc.rights.none.fl_str_mv |
open access http://purl.org/coar/access_right/c_abf2 Atribución 3.0 España https://creativecommons.org/licenses/by/3.0/es/ |
| dc.rights.openaire.fl_str_mv |
info:eu-repo/semantics/openAccess |
| rights_invalid_str_mv |
open access http://purl.org/coar/access_right/c_abf2 Atribución 3.0 España https://creativecommons.org/licenses/by/3.0/es/ |
| eu_rights_str_mv |
openAccess |
| dc.format.none.fl_str_mv |
application/pdf |
| dc.publisher.none.fl_str_mv |
MDPI |
| publisher.none.fl_str_mv |
MDPI |
| dc.source.none.fl_str_mv |
reponame:Docta Complutense instname:Universidad Complutense de Madrid (UCM) |
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Universidad Complutense de Madrid (UCM) |
| reponame_str |
Docta Complutense |
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Docta Complutense |
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|
| repository.mail.fl_str_mv |
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1869422837390901248 |
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15,301603 |