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

Molecules

卷:22

Mahabir P. Gupta¹  Eduardo Muñoz²  Rocío Sancho²  Luis M. Bedoya³  José Alcamí³  José Luis López-Pérez⁴  Dionisio A. Olmedo⁴  Esther del Olmo⁴  Arturo San Feliciano⁴ 

[1] CIFLORPAN, Center for Pharmacognostic Research on Panamanian Flora, College of Pharmacy, University of Panama, P.O. Box 0824-00172 Panama, Panama;

[2] Department of Cellular Biology, Physiology and Immunology, University of Córdoba, Faculty of Medicine Avda de Menendez Pidal s/n, 14004 Córdoba, Spain;

[3] National Centre of Microbiology, Institute Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain;

[4] Pharmaceutical Chemistry Area, Department of Pharmaceutical Sciences, University of Salamanca, Faculty of Pharmacy, CIETUS, IBSAL, Campus Miguel de Unamuno, 37007 Salamanca, Spain;

关键词: neoflavonoids;    4-phenyl-chromen-one;    AIDS;    Tat protein;    NF-κB inhibition;    anti-HIV activity;   

DOI  :  10.3390/molecules22020321

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown