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Merck
  • HIV-1 antiviral behavior of anionic PPI metallo-dendrimers with EDA core.

HIV-1 antiviral behavior of anionic PPI metallo-dendrimers with EDA core.

European journal of medicinal chemistry (2015-05-26)
Sandra García-Gallego, Laura Díaz, José Luis Jiménez, Rafael Gómez, F Javier de la Mata, M Ángeles Muñoz-Fernández
摘要

The development of novel strategies to prevent HIV-1 infection is of outstanding relevance. Metal complexes of Cu(2+), Ni(2+), Co(2+) and Zn(2+) derived from sulfonated and carboxylated poly(propylene imine) dendrimers with ethylenediamine core were evaluated as tunable antiviral agents against HIV-1. After demonstrating their biocompatibility, specific trends in the antiviral properties were found, related to both the dendritic scaffold (peripheral group, generation) and the bound metal ions (sort, amount). In HEC-1A and VK-2 cell lines, as model of the first barrier against HIV-1 infection, a high preventive inhibitory action was found, which also avoided virus internalization inside cells and inhibited both CCR5 and CXCR4 HIV-1 strains. In peripheral blood mononuclear cells (PBMC), as model of the second barrier, a dual preventive and therapeutic behavior was observed. A rational design of such metallodendrimers opens new avenues for the production of versatile and efficient treatments against HIV-1 infection.

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