Please use this identifier to cite or link to this item:http://hdl.handle.net/20.500.12105/7183
Title
Neoflavonoids as Inhibitors of HIV-1 Replication by Targeting the Tat and NF-κB Pathways
Author(s)
Olmedo, Dionisio A | López-Pérez, José Luis | Del Olmo, Esther | Bedoya, Luis M ISCIII | Sancho, Rocío | Alcamí, José ISCIII | Muñoz, Eduardo | Feliciano, Arturo San | Gupta, Mahabir P
Date issued
2017-02-19
Citation
Molecules. 2017 Feb 19;22(2). pii: E321.
Language
Inglés
Document type
journal article
Abstract
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.
Subject
MESH
Anti-HIV Agents | Biflavonoids | HIV Infections | HIV-1 | Humans | Microbial Sensitivity Tests | Molecular Structure | NF-kappa B | Signal Transduction | Virus Replication | tat Gene Products, Human Immunodeficiency Virus
Online version
DOI
Collections