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Article

Antioxidant Activity of Deferasirox and Its Metal Complexes in Model Systems of Oxidative Damage: Comparison with Deferiprone

1
Institute of Chemical Kinetics & Combustion, 630090 Novosibirsk, Russia
2
Postgraduate Research Institute of Science, Technology, Environment and Medicine, Limassol CY-3021, Cyprus
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Author to whom correspondence should be addressed.
Academic Editors: José Pinela, Lillian Barros and Maria Ines Dias
Molecules 2021, 26(16), 5064; https://doi.org/10.3390/molecules26165064
Received: 3 July 2021 / Revised: 17 August 2021 / Accepted: 18 August 2021 / Published: 20 August 2021
(This article belongs to the Special Issue Measurement of Antioxidant Activity: Advances and Perspectives)
Deferasirox is an orally active, lipophilic iron chelating drug used on thousands of patients worldwide for the treatment of transfusional iron overload. The essential transition metals iron and copper are the primary catalysts of reactive oxygen species and oxidative damage in biological systems. The redox effects of deferasirox and its metal complexes with iron, copper and other metals are of pharmacological, toxicological, biological and physiological importance. Several molecular model systems of oxidative damage caused by iron and copper catalysis including the oxidation of ascorbic acid, the peroxidation of linoleic acid micelles and the oxidation of dihydropyridine have been investigated in the presence of deferasirox using UV-visible and NMR spectroscopy. Deferasirox has shown antioxidant activity in all three model systems, causing substantial reduction in the rate of oxidation and oxidative damage. Deferasirox showed the greatest antioxidant activity in the oxidation of ascorbic acid with the participation of iron ions and reduced the reaction rate by about a 100 times. Overall, deferasirox appears to have lower affinity for copper in comparison to iron. Comparative studies of the antioxidant activity of deferasirox and the hydrophilic oral iron chelating drug deferiprone in the peroxidation of linoleic acid micelles showed lower efficiency of deferasirox in comparison to deferiprone. View Full-Text
Keywords: deferasirox; deferiprone; antioxidant activity; iron chelation; copper chelation; Fenton reaction; lipid peroxidation; ascorbic acid; linoleic acid; dihydropyridine; NMR deferasirox; deferiprone; antioxidant activity; iron chelation; copper chelation; Fenton reaction; lipid peroxidation; ascorbic acid; linoleic acid; dihydropyridine; NMR
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MDPI and ACS Style

Timoshnikov, V.A.; Kichigina, L.A.; Selyutina, O.Y.; Polyakov, N.E.; Kontoghiorghes, G.J. Antioxidant Activity of Deferasirox and Its Metal Complexes in Model Systems of Oxidative Damage: Comparison with Deferiprone. Molecules 2021, 26, 5064. https://doi.org/10.3390/molecules26165064

AMA Style

Timoshnikov VA, Kichigina LA, Selyutina OY, Polyakov NE, Kontoghiorghes GJ. Antioxidant Activity of Deferasirox and Its Metal Complexes in Model Systems of Oxidative Damage: Comparison with Deferiprone. Molecules. 2021; 26(16):5064. https://doi.org/10.3390/molecules26165064

Chicago/Turabian Style

Timoshnikov, Viktor A., Lilia A. Kichigina, Olga Y. Selyutina, Nikolay E. Polyakov, and George J. Kontoghiorghes 2021. "Antioxidant Activity of Deferasirox and Its Metal Complexes in Model Systems of Oxidative Damage: Comparison with Deferiprone" Molecules 26, no. 16: 5064. https://doi.org/10.3390/molecules26165064

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