Advertisement

 

 

Efficacy of carbosilane dendrimers with an antiretroviral combination against HIV-1 in the presence of semen-derived enhancer of viral infection.

Efficacy of carbosilane dendrimers with an antiretroviral combination against HIV-1 in the presence of semen-derived enhancer of viral infection.
Author Information (click to view)

García-Broncano P, Ceña-Diez R, de la Mata FJ, Gómez R, Resino S, Muñoz-Fernández MÁ,


García-Broncano P, Ceña-Diez R, de la Mata FJ, Gómez R, Resino S, Muñoz-Fernández MÁ, (click to view)

García-Broncano P, Ceña-Diez R, de la Mata FJ, Gómez R, Resino S, Muñoz-Fernández MÁ,

Advertisement
Share on FacebookTweet about this on TwitterShare on LinkedIn

European journal of pharmacology 2017 05 31811() 155-163 pii 10.1016/j.ejphar.2017.05.060

Abstract

Amyloid fibrils, which are present in semen, were considered to be a cause of topical vaginal gel ineffectiveness in vivo after microbicides failed as HIV-1 prophylaxis. Therefore, it was necessary to determine whether a dendrimer was suitable for further evaluation in an in vitro model of semen-enhanced viral infection (SEVI). We demonstrated that SEVI in TZM.bl cell cultures increased the infectivity of R5-HIV-1NL(AD8), pTHRO.c and pCH058.c isolates, causing higher IC50 values for two polyanionic carbosilane dendrimers, G2-STE16 and G3-S16. However, both dendrimers maintained protection rates of 90% at non-toxic concentrations. When dendrimers were combined with Tenofovir/Maraviroc (TDF/MVC), the anti-HIV-1 effect remained at a minimum IC50 increase between 1- and 7-fold in the presence of amyloid fibrils. In peripheral blood mononuclear cells (PBMC), IC50 values were slightly influenced by the presence of semen. In brief, dendrimers combined with antiretrovirals showed a synergistic effect. This result plays a crucial role in new microbicide formulations, as it overcomes the negative effects of amyloid fibrils.

Submit a Comment

Your email address will not be published. Required fields are marked *

fourteen + thirteen =

[ HIDE/SHOW ]