Intracellular Iron Binding and Antioxidant Activity of Phytochelators.

Abstract

Phytochelators have been studied as templates for designing new drugs for chelation therapy. This work evaluated key chemical and biological properties of five candidate phytochelators for iron overload diseases: maltol, mimosine, morin, tropolone, and esculetin. Intra- and extracellular iron affinity and antioxidant activity, as well as the ability to scavenge iron from holo-transferrin, were studied in physiologically relevant settings. Tropolone and mimosine (and, to a lesser extent, maltol) presented good binding capacity for iron, removing it from calcein, a high-affinity fluorescent probe. Tropolone and mimosine arrested iron-mediated oxidation of ascorbate with the same efficiency as the standard iron chelator DFO. Also, both were cell permeant and able to access labile pools of iron in HeLa and HepG2 cells. Mimosine was an effective antioxidant in cells stressed by iron and peroxide, being as efficient as the cell-permeant iron chelator deferiprone. These results reinforce the potential of those molecules, especially mimosine, as adjuvants in treatments for iron overload.

• Authors: Fredson Torres Silva, Breno Pannia Espósito
• Journal: Biological trace element research (Biol Trace Elem Res) Vol. 200 Issue 8 Pg. 3910-3918 (Aug 2022) ISSN: 1559-0720 [Electronic] United States
• PMID: 34648123 (Publication Type: Journal Article)
• Copyright: © 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

Chemical References

• Antioxidants
• Iron Chelating Agents
• Pyridones
• Mimosine
• Tropolone
• Iron
• Deferoxamine

Topics

• Antioxidants (pharmacology, therapeutic use)
• Deferoxamine
• Humans
• Iron (metabolism)
• Iron Chelating Agents (pharmacology)
• Iron Overload
• Mimosine (therapeutic use)
• Pyridones (therapeutic use)
• Tropolone (therapeutic use)