Jump to main content
Jump to site search

Issue 19, 2018
Previous Article Next Article

Sulfonate-ended carbosilane dendrimers with a flexible scaffold cause inactivation of HIV-1 virions and gp120 shedding

Author affiliations

Abstract

Infection with human immunodeficiency virus type 1 (HIV-1) continues to be a global public health issue, especially in low-resource countries. Sexual transmission is responsible for the majority of HIV-1 infections worldwide. Women are more susceptible to HIV-1 acquisition than men and represent nearly 50% of the HIV-infected population. Topical vaginal microbicides that act at the earlier stages of infection offer a prevention strategy to reduce the acquisition of HIV-1. Dendrimers are nano-sized, radially symmetric molecules with a well-defined and monodisperse structure consisting of tree-like arms or branches. We perform a TZM.bl cell line-based screening of two families of carbosilane dendrimers (6 nanocompounds: G1-S12P, G2-S24P, G3-S48P, G1-C12P, G2-C24P and G3-C48P) that we have previously synthesized, containing 12, 24 or 48 sulfonate (or carboxylate) end-groups and a polyphenolic core. This work shows that second- and third-generation sulfonate-ended carbosilane dendrimers with a polyphenolic core (G2-S24P and G3-S48P, respectively) display low cytotoxicity (CC50 > 300 μM) with virucidal anti-R5-HIV-1 activity (EC50 < 50 nM; therapeutic index >6000) causing irreversible HIV-1 inactivation (80–90%) by loss of HIV-1 RNA (40%), gp120 shedding (70–80%) and p24 capsid protein release (45–60%). Herein, we demonstrate that sulfonate end-groups and a flexible scaffold from carbosilane dendrimers strongly influence their properties acting as potent virucides.

Graphical abstract: Sulfonate-ended carbosilane dendrimers with a flexible scaffold cause inactivation of HIV-1 virions and gp120 shedding

Back to tab navigation

Supplementary files

Publication details

The article was received on 27 Feb 2018, accepted on 07 Apr 2018 and first published on 09 Apr 2018


Article type: Paper
DOI: 10.1039/C8NR01664J
Citation: Nanoscale, 2018,10, 8998-9011
  •   Request permissions

    Sulfonate-ended carbosilane dendrimers with a flexible scaffold cause inactivation of HIV-1 virions and gp120 shedding

    D. Sepúlveda-Crespo, F. J. de la Mata, R. Gómez and M. A. Muñoz-Fernández, Nanoscale, 2018, 10, 8998
    DOI: 10.1039/C8NR01664J

Search articles by author

Spotlight

Advertisements