Structural modulation of the biological activity of gold nanoparticles functionalized with a carbonic anhydrase inhibitor

  • Francesca Bellissima
  • Fabrizio Carta
  • Alessio Innocenti
  • Andrea Scozzafava
  • Piero Baglioni
  • Claudiu T. Supuran
  • Debora Berti
Regular Article


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 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.

Graphical abstract


Soft Matter: Colloids and Nanoparticles 

List of abbreviations


gold nanoparticles


carbonic anhydrase




carbonic anhydrase inhibitor




dynamic light scattering


small angle X-ray scattering


attenuated total reflection Fourier-transformed infrared spectroscopy


trisodium citrate dihydrate


inductively coupled plasma-atomic emission spectroscopy


thermogravimetric analysis


scattering length density


transmission electron microscopy


surface plasmon resonance


Derjaguin, Landau, Verwey, Overbeek


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Copyright information

© EDP Sciences, SIF, Springer-Verlag Berlin Heidelberg 2013

Authors and Affiliations

  • Francesca Bellissima
    • 1
  • Fabrizio Carta
    • 1
  • Alessio Innocenti
    • 1
  • Andrea Scozzafava
    • 1
  • Piero Baglioni
    • 1
  • Claudiu T. Supuran
    • 1
  • Debora Berti
    • 1
  1. 1.Department of Chemistry and CSGIUniversity of FlorenceFlorenceItaly

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