title: Phenylboronic-acid-modified nanoparticles: potential antiviral therapeutics.
abstract: Phenylboronic-acid-modified nanoparticles (NPs) are attracting considerable attention for biological and biomedical applications. We describe here a convenient and general protocol for attaching multiple copies of para-substituted phenylboronic acid moieties onto either iron-oxide-, silica- or diamond-derived NPs. The boronic acid functionalized NPs are all fabricated by first modifying the surface of each particle type with 4-azidobenzoic ester functions. These azide-terminated nanostructures were then reacted with 4-[1-oxo-4-pentyn-1-yl) amino]phenylboronic acid units via a Cu(I) catalyzed Huisgen cycloaddition to furnish, conveniently, the corresponding boronic-acid modified NPs (or "borono-lectins") targeted in this work. The potential of these novel "borono-lectins" as antiviral inhibitors was investigated against the Hepatitis C virus (HCV) exploiting a bioassay that measures the potential of drugs to interfere with the ability of cell-culture-derived JFH1 virus particles to infect healthy hepatocytes. As far as we are aware, this is the first report that describes NP-derived viral entry inhibitors and thus serves as a "proof-of-concept" study. The novel viral entry activity demonstrated, and the fact that the described boronic-acid-functionalized NPs all display much reduced cellular toxicities compared with alternate NPs, sets the stage for their further investigation. The data supports that NP-derived borono-lectins should be pursued as a potential therapeutic strategy for blocking viral entry of HCV.
authors.affiliation: Institut de Recherche Interdisciplinaire (IRI, USR CNRS 3078), Université Lille 1 , Parc de la Haute Borne, 50 Avenue de Halley, BP 70478, 59658 Villeneuve d'Ascq, France.
authors.forename: Manakamana
authors.initials: M
authors.lastname: Khanal
authors.forename: Thibaut
authors.initials: T
authors.lastname: Vausselin
authors.forename: Alexandre
authors.initials: A
authors.lastname: Barras
authors.forename: Omprakash
authors.initials: O
authors.lastname: Bande
authors.forename: Kostiantyn
authors.initials: K
authors.lastname: Turcheniuk
authors.forename: Mohammed
authors.initials: M
authors.lastname: Benazza
authors.forename: Vladimir
authors.initials: V
authors.lastname: Zaitsev
authors.forename: Cristian Mihail
authors.initials: CM
authors.lastname: Teodorescu
authors.forename: Rabah
authors.initials: R
authors.lastname: Boukherroub
authors.forename: Aloysius
authors.initials: A
authors.lastname: Siriwardena
authors.forename: Jean
authors.initials: J
authors.lastname: Dubuisson
authors.forename: Sabine
authors.initials: S
authors.lastname: Szunerits
mesh_terms: D000998:Antiviral Agents / Q000494:pharmacology*; D001897:Boronic Acids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D053758:Nanoparticles; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000998:Antiviral Agents; D001897:Boronic Acids; C010686:benzeneboronic acid