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

• The development of novel strategies to prevent HIV-1 infection is of outstanding relevance. Metal complexes of Cu2+, Ni2+, Co2+ and Zn2+ 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.

Subject headings

MEDICIN OCH HÄLSOVETENSKAP  -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)

MEDICAL AND HEALTH SCIENCES  -- Basic Medicine -- Medicinal Chemistry (hsv//eng)

Keyword

Carboxylate

Dendrimer

HIV

Sulfonate

Transition metal

anti human immunodeficiency virus agent

chemokine receptor CCR5

chemokine receptor CXCR4

cobalt complex

copper complex

enfuvirtide

ethylenediamine

galactosylceramide

nickel complex

plerixafor

poly(propyleneimine)

polypropylene

suramin

tenofovir

unclassified drug

zinc complex

antiviral activity

Article

binding affinity

biocompatibility

carboxylation

complex formation

conformational transition

controlled study

female

human

human cell

Human immunodeficiency virus 1

Human immunodeficiency virus 1 infection

in vitro study

internalization

nonhuman

peripheral blood mononuclear cell

sulfonation

tropism

virus entry

virus inhibition

virus particle

virus strain

Publication and Content Type

ref (subject category)

art (subject category)