Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects
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Date
2020-04-28Author
Navas, Arturo
Jannus, Fatin
Fernández, Belén
Cepeda Ruiz, Javier
Medina O’Donnell, Marta
Díaz Ruiz, Luis
Sánchez González, Cristina
Llopis, Juan
Rufino Palomares, E.
Lupiáñez, José Antonio
Quiles, José Luis
Battino, Maurizio
Choquesillo Lazarte, Duane
Ruiz Muelle, Ana Belén
Fernández, Ignacio
Reyes Zurita, Fernando
Rodríguez Diéguez, Antonio
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International Journal of Molecular Sciences 21(9) : (2020) // Article ID 3146
Abstract
We have designed and synthesized two novel cobalt coordination compounds using bumetanide (bum) and indomethacin (ind) therapeutic agents. The anti-inflammatory effects of cobalt metal complexes with ind and bum were assayed in lipopolysaccharide stimulated RAW 264.7 macrophages by inhibition of nitric oxide production. Firstly, we determined the cytotoxicity and the anti-inflammatory potential of the cobalt compounds and ind and bum ligands in RAW 264.7 cells. Indomethacin-based metal complex was able to inhibit the NO production up to 35% in a concentration-dependent manner without showing cytotoxicity, showing around 6–37 times more effective than indomethacin. Cell cycle analysis showed that the inhibition of NO production was accompanied by a reversion of the differentiation processes in LPS-stimulated RAW 264.7 cells, due to a decreased of cell percentage in G0/G1 phase, with the corresponding increase in the number of cells in S phase. These two materials have mononuclear structures and show slow relaxation of magnetization. Moreover, both compounds show anti-diabetic activity with low in vitro cell toxicities. The formation of metal complexes with bioactive ligands is a new and promising strategy to find new compounds with high and enhanced biochemical properties and promises to be a field of great interest.
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Except where otherwise noted, this item's license is described as 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).