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Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies
Copper-based compounds are promising entities for target-specific next-generation anticancer and NSAIDS therapeutics. In lieu of this, benzimidazole scaffold plays an important role, because of their wide variety of potential functionalizations and coordination modes. Herein, we report three copper...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Nature Publishing Group UK
2019
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6437194/ https://www.ncbi.nlm.nih.gov/pubmed/30918270 http://dx.doi.org/10.1038/s41598-019-41063-x |
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author | Hussain, Afzal AlAjmi, Mohamed Fahad Rehman, Md. Tabish Amir, Samira Husain, Fohad Mabood Alsalme, Ali Siddiqui, Maqsood Ahmad AlKhedhairy, Abdulaziz A. Khan, Rais Ahmad |
author_facet | Hussain, Afzal AlAjmi, Mohamed Fahad Rehman, Md. Tabish Amir, Samira Husain, Fohad Mabood Alsalme, Ali Siddiqui, Maqsood Ahmad AlKhedhairy, Abdulaziz A. Khan, Rais Ahmad |
author_sort | Hussain, Afzal |
collection | PubMed |
description | Copper-based compounds are promising entities for target-specific next-generation anticancer and NSAIDS therapeutics. In lieu of this, benzimidazole scaffold plays an important role, because of their wide variety of potential functionalizations and coordination modes. Herein, we report three copper complexes 1–3 with benzimidazole-derived scaffolds, a biocompatible molecule, and secondary ligands viz, 1–10-phenanthroline and 2,2′-bipyridyl. All the copper complexes have been designed, synthesized and adequately characterized using various spectroscopic techniques. In-vitro, human serum albumin (HSA) binding was also carried out using fluorescence technique and in-silico molecular modeling studies, which exhibited significant binding affinities of the complexes with HSA. Furthermore, copper complexes 1–3 were tested for biological studies, i.e., anticancer as well as NSAIDS. In vitro cytotoxicity results were carried out on cultured MCF-7 cell lines. To get the insight over the mechanism of action, GSH depletion and change in lipid peroxidation were tested and thus confirmed the role of ROS generation, responsible for the cytotoxicity of the complexes 1–3. Moreover, the copper complexes 1–3 were tested for potential to act as NSAIDS on albino rats and mice in animal studies in-vivo. Additionally, we also predicted the mechanism of action of the copper complexes 1–3 using molecular modeling studies with COX-2 inhibitor. |
format | Online Article Text |
id | pubmed-6437194 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | Nature Publishing Group UK |
record_format | MEDLINE/PubMed |
spelling | pubmed-64371942019-04-03 Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies Hussain, Afzal AlAjmi, Mohamed Fahad Rehman, Md. Tabish Amir, Samira Husain, Fohad Mabood Alsalme, Ali Siddiqui, Maqsood Ahmad AlKhedhairy, Abdulaziz A. Khan, Rais Ahmad Sci Rep Article Copper-based compounds are promising entities for target-specific next-generation anticancer and NSAIDS therapeutics. In lieu of this, benzimidazole scaffold plays an important role, because of their wide variety of potential functionalizations and coordination modes. Herein, we report three copper complexes 1–3 with benzimidazole-derived scaffolds, a biocompatible molecule, and secondary ligands viz, 1–10-phenanthroline and 2,2′-bipyridyl. All the copper complexes have been designed, synthesized and adequately characterized using various spectroscopic techniques. In-vitro, human serum albumin (HSA) binding was also carried out using fluorescence technique and in-silico molecular modeling studies, which exhibited significant binding affinities of the complexes with HSA. Furthermore, copper complexes 1–3 were tested for biological studies, i.e., anticancer as well as NSAIDS. In vitro cytotoxicity results were carried out on cultured MCF-7 cell lines. To get the insight over the mechanism of action, GSH depletion and change in lipid peroxidation were tested and thus confirmed the role of ROS generation, responsible for the cytotoxicity of the complexes 1–3. Moreover, the copper complexes 1–3 were tested for potential to act as NSAIDS on albino rats and mice in animal studies in-vivo. Additionally, we also predicted the mechanism of action of the copper complexes 1–3 using molecular modeling studies with COX-2 inhibitor. Nature Publishing Group UK 2019-03-27 /pmc/articles/PMC6437194/ /pubmed/30918270 http://dx.doi.org/10.1038/s41598-019-41063-x Text en © The Author(s) 2019 Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/. |
spellingShingle | Article Hussain, Afzal AlAjmi, Mohamed Fahad Rehman, Md. Tabish Amir, Samira Husain, Fohad Mabood Alsalme, Ali Siddiqui, Maqsood Ahmad AlKhedhairy, Abdulaziz A. Khan, Rais Ahmad Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title | Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title_full | Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title_fullStr | Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title_full_unstemmed | Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title_short | Copper(II) complexes as potential anticancer and Nonsteroidal anti-inflammatory agents: In vitro and in vivo studies |
title_sort | copper(ii) complexes as potential anticancer and nonsteroidal anti-inflammatory agents: in vitro and in vivo studies |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6437194/ https://www.ncbi.nlm.nih.gov/pubmed/30918270 http://dx.doi.org/10.1038/s41598-019-41063-x |
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