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

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. 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 well-defined and monodisperse structure consisting of tree-like arms or branches. We perform a screening from two families of carbosilane dendrimers (6 nanocompounds) that we have previously synthesized, possessing 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 a virucidal antiviral activity (EC50 < 50 nM; therapeutic index > 5,000) causing irreversible HIV-1 inactivation by targeting Env protein, membrane disruption, loss of HIV-1 RNA, gp120 shedding and p24 capsid protein release. Herein, we demonstrate that sulfonate end-groups and a flexible scaffold from carbosilane dendrimers strongly influence their properties acting as potent virucides.

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

    D. Sepúlveda-Crespo, J. de la Mata, R. Gómez Ramírez and M. Á. Muñoz-Fernández, Nanoscale, 2018, Accepted Manuscript , DOI: 10.1039/C8NR01664J

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