title: Structural modulation of the biological activity of gold nanoparticles functionalized with a carbonic anhydrase inhibitor.
abstract: Gold nanoparticles (AuNPs) have gained attention for their potential and application in different fields, e.g. nanomedicine. This study explores the surface functionalization of AuNP with inhibitors of carbonic anhydrases (CAs, EC 4.2.1.1). Some CA transmembrane isoforms have been recognized as therapeutic targets for the treatment of hypoxic tumors. Embedding a CA inhibitory function onto a nanosized unit has been proved to enable selective targeting of transmembrane isoforms. We report the preparation in aqueous media, the characterization and CA inhibition tests of AuNPs coated with a sulfonamide (SA) derivative, already known for its inhibitory activity toward CAs. The physico-chemical characterization of SA-coated AuNPs was performed with a combination of scattering and spectroscopic techniques. We detect a threshold effect of the SA concentration on the final hydrodynamic and core sizes of the capped nanoparticles and on their stability over aggregation. These modified nanoparticles were assayed for inhibition of some CA transmembrane isoforms (CA IX and XII) as well as of two cytosolic isoforms (CA I and II), and show interesting inhibitory efficiency in the submicromolar range and some selectivity for transmembrane isoforms.
authors.affiliation: Department of Chemistry and CSGI, University of Florence, Sesto Fiorentino, 50019, Florence, Italy.
authors.forename: Francesca
authors.initials: F
authors.lastname: Bellissima
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Carta
authors.forename: Alessio
authors.initials: A
authors.lastname: Innocenti
authors.forename: Andrea
authors.initials: A
authors.lastname: Scozzafava
authors.forename: Piero
authors.initials: P
authors.lastname: Baglioni
authors.forename: Claudiu T
authors.initials: CT
authors.lastname: Supuran
authors.forename: Debora
authors.initials: D
authors.lastname: Berti
mesh_terms: D002257:Carbonic Anhydrase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000187:drug effects; D006046:Gold / Q000737:chemistry*; D053768:Metal Nanoparticles / Q000737:chemistry*; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D013449:Sulfonamides; D006046:Gold; D002256:Carbonic Anhydrases