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Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects
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 nit...
Autores principales: | , , , , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7246571/ https://www.ncbi.nlm.nih.gov/pubmed/32365648 http://dx.doi.org/10.3390/ijms21093146 |
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author | Navas, Arturo Jannus, Fatin Fernández, Belén Cepeda, Javier Medina O’Donnell, Marta Díaz-Ruiz, Luis Sánchez-González, Cristina Llopis, Juan Seco, José M. Rufino-Palomares, E. Lupiáñez, José Antonio Gómez-Ruiz, Santiago Quiles, José Luis Battino, Maurizio Choquesillo-Lazarte, Duane Ruiz-Muelle, Ana Belén Fernández, Ignacio Reyes-Zurita, Fernando Rodríguez-Diéguez, Antonio |
author_facet | Navas, Arturo Jannus, Fatin Fernández, Belén Cepeda, Javier Medina O’Donnell, Marta Díaz-Ruiz, Luis Sánchez-González, Cristina Llopis, Juan Seco, José M. Rufino-Palomares, E. Lupiáñez, José Antonio Gómez-Ruiz, Santiago Quiles, José Luis Battino, Maurizio Choquesillo-Lazarte, Duane Ruiz-Muelle, Ana Belén Fernández, Ignacio Reyes-Zurita, Fernando Rodríguez-Diéguez, Antonio |
author_sort | Navas, Arturo |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-7246571 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-72465712020-06-10 Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects Navas, Arturo Jannus, Fatin Fernández, Belén Cepeda, Javier Medina O’Donnell, Marta Díaz-Ruiz, Luis Sánchez-González, Cristina Llopis, Juan Seco, José M. Rufino-Palomares, E. Lupiáñez, José Antonio Gómez-Ruiz, Santiago Quiles, José Luis Battino, Maurizio Choquesillo-Lazarte, Duane Ruiz-Muelle, Ana Belén Fernández, Ignacio Reyes-Zurita, Fernando Rodríguez-Diéguez, Antonio Int J Mol Sci Article 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. MDPI 2020-04-29 /pmc/articles/PMC7246571/ /pubmed/32365648 http://dx.doi.org/10.3390/ijms21093146 Text en © 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/). |
spellingShingle | Article Navas, Arturo Jannus, Fatin Fernández, Belén Cepeda, Javier Medina O’Donnell, Marta Díaz-Ruiz, Luis Sánchez-González, Cristina Llopis, Juan Seco, José M. Rufino-Palomares, E. Lupiáñez, José Antonio Gómez-Ruiz, Santiago Quiles, José Luis Battino, Maurizio Choquesillo-Lazarte, Duane Ruiz-Muelle, Ana Belén Fernández, Ignacio Reyes-Zurita, Fernando Rodríguez-Diéguez, Antonio Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title | Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title_full | Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title_fullStr | Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title_full_unstemmed | Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title_short | Designing Single-Molecule Magnets as Drugs with Dual Anti-Inflammatory and Anti-Diabetic Effects |
title_sort | designing single-molecule magnets as drugs with dual anti-inflammatory and anti-diabetic effects |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7246571/ https://www.ncbi.nlm.nih.gov/pubmed/32365648 http://dx.doi.org/10.3390/ijms21093146 |
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