ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Development of a platform for the production of multiple modal chelating and imaging agents using desferrioxamine and bovine albumin as a model

Lucas Antonio Arias Correia, Rodrigo Santos Garcia, Caroline Cristiano Real, Daniel Henrique Uzueli, Ulisses Lacerda de Figueiredo Sá, Fabio Luiz Navarro Marques, Luiz Alberto Colnago, and Breno Pannia Espósito

Department of Fundamental Chemistry, University of São Paulo, São Paulo, Brazil

E-mail: breno@iq.usp.br

Received: 10 July 2020  Accepted: 22 September 2020

Abstract:

The linker p-SCN-Bz-desferrioxamine was used as a conjugating agent to bovine serum albumin. The conjugate (BSA-DFO) did not display relevant structural alterations in comparison with the native protein. BSA-DFO was able to bind iron in a high affinity, antioxidant form similar to the native siderophore desferrioxamine. The gadolinium complex of BSA-DFO displayed 7–10 times higher relaxivities compared to the low molecular weight complex. Preparation of the radiotracers ⁶⁸Ga(BSA-DFO) and ⁸⁹Zr(BSA-DFO) in high radiochemical yields was accomplished quickly in mild conditions. These results indicate that BSA-DFO might be useful as an alternative treatment for iron overload disorders, and as a platform for the production of radiotracers or contrast agents for magnetic resonance imaging.

Keywords: Desferrioxamine; Albumin; Iron; Gadolinium; Gallium-68; Zirconium-89

Full paper is available at www.springerlink.com.

DOI: 10.1007/s11696-020-01374-0

Chemical Papers 75 (3) 1157–1163 (2021)