POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation

POCOP-Ni(II) pincer compounds have primarily been explored as catalysts, but their potential biological activity has been scarcely studied. To address this gap, we evaluated the anticancer and antioxidant potential of four POCOP-Ni(II) complexes derived from phloroglucinol. A comprehensive supramole...

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Main Authors: Andrés Amaya-Flórez, Juan S. Serrano-García, Jordi Ruiz-Galindo, Antonino Arenaza-Corona, J. Antonio Cruz-Navarro, Adrian L. Orjuela, Jorge Alí-Torres, Marcos Flores-Alamo, Patricia Cano-Sanchez, Viviana Reyes-Márquez, David Morales-Morales
Format: Article
Language:English
Published: Frontiers Media S.A. 2024-11-01
Series:Frontiers in Chemistry
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Online Access:https://www.frontiersin.org/articles/10.3389/fchem.2024.1483999/full
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author Andrés Amaya-Flórez
Juan S. Serrano-García
Jordi Ruiz-Galindo
Antonino Arenaza-Corona
J. Antonio Cruz-Navarro
Adrian L. Orjuela
Jorge Alí-Torres
Marcos Flores-Alamo
Patricia Cano-Sanchez
Viviana Reyes-Márquez
David Morales-Morales
author_facet Andrés Amaya-Flórez
Juan S. Serrano-García
Jordi Ruiz-Galindo
Antonino Arenaza-Corona
J. Antonio Cruz-Navarro
Adrian L. Orjuela
Jorge Alí-Torres
Marcos Flores-Alamo
Patricia Cano-Sanchez
Viviana Reyes-Márquez
David Morales-Morales
author_sort Andrés Amaya-Flórez
collection DOAJ
description POCOP-Ni(II) pincer compounds have primarily been explored as catalysts, but their potential biological activity has been scarcely studied. To address this gap, we evaluated the anticancer and antioxidant potential of four POCOP-Ni(II) complexes derived from phloroglucinol. A comprehensive supramolecular analysis, based on single-crystal X-ray diffraction (DRX) structures, was conducted using Hirshfeld surfaces and non-covalent interaction analysis. The cytotoxicity of all complexes was systematically assessed against various cancerous cell lines, as well as a non-cancerous cell line (COS-7). The results revealed that complexes 1b and 1c exhibited remarkable antiproliferative activity, with IC50 values ranging from 2.43 to 7.85 μM against cancerous cell lines U251, K562, HCT-15, MCF-7, and SK-LU-1. To further elucidate their mechanism of action, a competitive fluorescence displacement assay with ethidium bromide (EB) suggested that these complexes possess the ability to intercalate with DNA. This multifaceted investigation not only enhances our understanding of the biological potential of POCOP-Ni complexes but also provides valuable insights into their structural features and interactions, paving the way for future exploration in both catalytic and therapeutic domains.
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spelling doaj-art-f122df3ad1cc451486cb4e3ce0144ad02024-11-20T04:50:01ZengFrontiers Media S.A.Frontiers in Chemistry2296-26462024-11-011210.3389/fchem.2024.14839991483999POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluationAndrés Amaya-Flórez0Juan S. Serrano-García1Jordi Ruiz-Galindo2Antonino Arenaza-Corona3J. Antonio Cruz-Navarro4Adrian L. Orjuela5Jorge Alí-Torres6Marcos Flores-Alamo7Patricia Cano-Sanchez8Viviana Reyes-Márquez9David Morales-Morales10Instituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoDepartamento de Química, Universidad Nacional de Colombia-Sede Bogotá, Bogotá, ColombiaDepartamento de Química, Universidad Nacional de Colombia-Sede Bogotá, Bogotá, ColombiaFacultad de Química, División de Estudios de Posgrado, Universidad Nacional Autónoma de México, Mexico city, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoDepartamento de Ciencias Químico-Biológicas, Universidad de Sonora, Hermosillo, Sonora, MexicoInstituto de Química, Universidad Nacional Autónoma de México, Ciudad de México, MexicoPOCOP-Ni(II) pincer compounds have primarily been explored as catalysts, but their potential biological activity has been scarcely studied. To address this gap, we evaluated the anticancer and antioxidant potential of four POCOP-Ni(II) complexes derived from phloroglucinol. A comprehensive supramolecular analysis, based on single-crystal X-ray diffraction (DRX) structures, was conducted using Hirshfeld surfaces and non-covalent interaction analysis. The cytotoxicity of all complexes was systematically assessed against various cancerous cell lines, as well as a non-cancerous cell line (COS-7). The results revealed that complexes 1b and 1c exhibited remarkable antiproliferative activity, with IC50 values ranging from 2.43 to 7.85 μM against cancerous cell lines U251, K562, HCT-15, MCF-7, and SK-LU-1. To further elucidate their mechanism of action, a competitive fluorescence displacement assay with ethidium bromide (EB) suggested that these complexes possess the ability to intercalate with DNA. This multifaceted investigation not only enhances our understanding of the biological potential of POCOP-Ni complexes but also provides valuable insights into their structural features and interactions, paving the way for future exploration in both catalytic and therapeutic domains.https://www.frontiersin.org/articles/10.3389/fchem.2024.1483999/fullcytotoxic evaluationantioxidant propertiespincer compoundsPOCOP-Ni(II) complexesmetallopharmaceuticals
spellingShingle Andrés Amaya-Flórez
Juan S. Serrano-García
Jordi Ruiz-Galindo
Antonino Arenaza-Corona
J. Antonio Cruz-Navarro
Adrian L. Orjuela
Jorge Alí-Torres
Marcos Flores-Alamo
Patricia Cano-Sanchez
Viviana Reyes-Márquez
David Morales-Morales
POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
Frontiers in Chemistry
cytotoxic evaluation
antioxidant properties
pincer compounds
POCOP-Ni(II) complexes
metallopharmaceuticals
title POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
title_full POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
title_fullStr POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
title_full_unstemmed POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
title_short POCOP-Ni(II) pincer compounds derived from phloroglucinol. Cytotoxic and antioxidant evaluation
title_sort pocop ni ii pincer compounds derived from phloroglucinol cytotoxic and antioxidant evaluation
topic cytotoxic evaluation
antioxidant properties
pincer compounds
POCOP-Ni(II) complexes
metallopharmaceuticals
url https://www.frontiersin.org/articles/10.3389/fchem.2024.1483999/full
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