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.

Highlights

  • The special interest in deferoxamine B (DFOB) derives from its important pharmacological role for patients with blood diseases that depend on transfusions and hemochromatosis

  • Ascorbic acid plays an important role in DFOB-ICT and it is considered as a standard adjuvant therapy: several studies highlight that the administration of oral ascorbate in combination with subcutaneous DFOB causes a substantial increase in iron excretion [47,48,49]

  • The reported thermodynamic data highlight the potential use of DFOB as an effective metal chelator, for the Fe(III) ion, and for many other cations, including several transition, lanthanoid and actinoid metal ions

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Summary

Introduction

Once the complex between the siderophore and Fe(III) is formed, it returns to the generating cell through specific recognition pathways that include surface proteins capable of activating an import sequence. The special interest in DFOB derives from its important pharmacological role for patients with blood diseases that depend on transfusions (such as β-thalassemia major) and hemochromatosis. These patients must regularly assume DFOB (marketed under the trade name Desferal® ), either alone or in combination with other drugs, to remove excess iron due to the hemolysis of blood cells.

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