Deferoxamine B: A Natural, Excellent and Versatile Metal Chelator

Abstract

Deferoxamine B is an outstanding molecule which has been widely studied in the past decade for its ability to bind iron and many other metal ions. The versatility of this metal chelator makes it suitable for a number of medicinal and analytical applications, from the well-known iron chelation therapy to the most recent use in sensor devices. The three bidentate hydroxamic functional groups of deferoxamine B are the centerpiece of its metal binding ability, which allows the formation of stable complexes with many transition, lanthanoid and actinoid metal ions. In addition to the ferric ion, in fact, more than 20 different metal complexes of deferoxamine b have been characterized in terms of their chemical speciation in solution. In addition, the availability of a terminal amino group, most often not involved in complexation, opens the way to deferoxamine B modification and functionalization. This review aims to collect and summarize the available data concerning the complex-formation equilibria in solutions of deferoxamine B with different metal ions. A general overview of the progress of its applications over the past decade is also discussed, including the treatment of iron overload-associated diseases, its clinical use against cancer and neurodegenerative disorders and its role as a diagnostic tool.

Metal Coordination Properties of a Chromophoric Desferrioxamine (DFO) Derivative: Insight on the Coordination Stoichiometry and Thermodynamic Stability of Zr4+ Complexes

“…The determined protonation constants are listed in Table 1 . Similar to DFO [ 26 ], DFO–Pm is also involved in four protonation equilibria occurring in the alkaline region ( Figure S1 in Supplementary Materials ), but the latter, unlike DFO, undergoes a fifth protonation in acidic media (pH < 4).…”

“…The complex species formed and the corresponding stability constants were determined by computer analysis of the potentiometric titration data (0.1 M Me 4 NCl, 298.15 K), performed with the Hyperquad [ 27 ] program, are reported in Table 1 . Despite DFO complexes with more than 20 different metal ions have been characterized in terms of their chemical speciation in solution, the alkaline metal cations appear to have been forgotten [ 26 ]. To partially remedy this shortcoming, we also turned our interests toward the complexation equilibria of DFO with Na + and K + and determined the corresponding stability constants, which have also been included in Table 1 .…”

“…The stability constants of the DFO complexes have been determined by different authors under relatively different temperature and ionic strength conditions. These constants were recently collected in a review paper that offers a rapid and clear overview of this ligand’s coordination properties [ 26 ]. A comparative analysis of the values that are available in the literature and of those determined in the present work ( Table 1 ) for DFO and DFO–Pm allows us to draw some general conclusions.…”

[68Ga]Ga-DFO-c(RGDyK): Synthesis and Evaluation of Its Potential for Tumor Imaging in Mice

“…Although DFO is well-accessible and an established chelating agent in nuclear medicine for peptide and particularly antibody radiolabeling, to our knowledge, DFO-based RGD peptides for radiometal labeling have not been studied yet. DFO is a molecule known for its ability to bind many different metal ions for years [ 27 ]. In 1968, it was also approved for medical use by the FDA under the brand name Desferal ® (Novartis, Basel, Switzerland) and became a well-established clinically used medication [ 16 ].…”

Desferrioxamine B-Mediated Pre-Clinical In Vivo Imaging of Infection by the Mold Fungus Aspergillus fumigatus

“…DFO-B (trade name Desferal ® ) is an approved drug that has been used in clinics for decades for metal chelation therapy in beta-thalassemia, sideroblastic anaemia, auto-immune haemolytic anemia and other iron or aluminum overload pathologies [ 18 , 19 , 20 ]. Recently, DFO-B-complexed 68 Ga ([ 68 Ga]Ga-DFO-B) was shown to be suitable for the molecular imaging of bacterial infections in animal infection models [ 21 ].…”