Inherent anti-HIV activity of biocompatible anionic citrate-PEG-citrate dendrimer

Mol Biol Rep. 2019 Feb;46(1):143-149. doi: 10.1007/s11033-018-4455-6. Epub 2018 Nov 9.

Abstract

The development of new combinations to empower better protection against HIV infection is particularly important. Anionic polymers can block HIV infection. In the current study, first generation (G1) and second generation (G2) novel water-soluble anionic citrate-PEG-citrate dendrimers were synthesized and characterized with Fourier-transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectroscopy (NMR), and dynamic light scattering (DLS) methods. After the biocompatibility of the G2 dendrimer was determined, its antiviral activity was evaluated. This function may contribute to the peripheral groups of this dendrimer (carboxylate group). In order to measure the inhibitory effect of G2 on HIV infection, both pre-treatment (treated with G2 dendrimer before HIV infection) and co-treatment (simultaneously treated with G2 dendrimer and HIV infection) were used in vitro. The results showed the good synthesis of the G2 dendrimer, and the dendrimer showed antiviral properties (ICC50:0.4 mM) and low toxicity (CC50:0.6 mM) at high concentrations. A strong inhibitory effect was found when the co-treatment approach was used. This study achieved promising results which encourage the use of G2 dendrimers as anti-HIV agents.

Keywords: Biocompatible; Dendrimer; HIV inhibition; Polyanionic polymer.

MeSH terms

  • Anti-HIV Agents / pharmacology
  • Citrates
  • Citric Acid / pharmacology*
  • Dendrimers / pharmacology
  • HIV Infections / drug therapy
  • HIV Infections / physiopathology
  • HIV-1 / drug effects*
  • Humans
  • Polyelectrolytes
  • Polyethylene Glycols / chemical synthesis
  • Polyethylene Glycols / pharmacology*
  • Polymers / pharmacology

Substances

  • Anti-HIV Agents
  • Citrates
  • Dendrimers
  • Polyelectrolytes
  • Polymers
  • polyanions
  • Citric Acid
  • Polyethylene Glycols