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Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity
A series of [RuCl(2)(p-cymene)(NHC)] complexes were obtained by reacting [RuCl(2)(p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9921063/ https://www.ncbi.nlm.nih.gov/pubmed/36771026 http://dx.doi.org/10.3390/molecules28031359 |
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author | Al Nasr, Ibrahim S. Koko, Waleed S. Khan, Tariq A. Gürbüz, Nevin Özdemir, Ismail Hamdi, Naceur |
author_facet | Al Nasr, Ibrahim S. Koko, Waleed S. Khan, Tariq A. Gürbüz, Nevin Özdemir, Ismail Hamdi, Naceur |
author_sort | Al Nasr, Ibrahim S. |
collection | PubMed |
description | A series of [RuCl(2)(p-cymene)(NHC)] complexes were obtained by reacting [RuCl(2)(p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the biological activities of these compounds as antienzymatic, antioxidant, antibacterial, anticancer, and antiparasitic agents. The results revealed that complexes 3b and 3d were the most potent inhibitors against AchE with IC(50) values of 2.52 and 5.06 μM mL(−1). Additionally, 3d proved very good antimicrobial activity against all examined microorganisms with IZ (inhibition zone) over 25 mm and MIC (minimum inhibitory concentration) < 4 µM. Additionally, the ligand 2a and its corresponding ruthenium (II) complex 3a had good cytotoxic activity against both cancer cells HCT-116 and HepG-2, with IC(50) values of (7.76 and 11.76) and (4.12 and 9.21) μM mL(−1), respectively. Evaluation of the antiparasitic activity of these complexes against Leishmania major promastigotes and Toxoplasma gondii showed that ruthenium complexes were more potent than the free ligand, with an IC(50) values less than 1.5 μM mL(−1). However, 3d was found the best one with SI (selectivity index) values greater than 5 so it seems to be the best candidate for antileishmanial drug discovery program, and much future research are recommended for mode of action and in vivo evaluation. In general, Ru-NHC complexes are the most effective against L. major promastigotes. |
format | Online Article Text |
id | pubmed-9921063 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-99210632023-02-12 Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity Al Nasr, Ibrahim S. Koko, Waleed S. Khan, Tariq A. Gürbüz, Nevin Özdemir, Ismail Hamdi, Naceur Molecules Article A series of [RuCl(2)(p-cymene)(NHC)] complexes were obtained by reacting [RuCl(2)(p-cymene)]2 with in situ generated Ag-N-heterocyclic carbene (NHC) complexes. The structure of the obtained complexes was determined by the appropriate spectroscopy and elemental analysis. In addition, we evaluated the biological activities of these compounds as antienzymatic, antioxidant, antibacterial, anticancer, and antiparasitic agents. The results revealed that complexes 3b and 3d were the most potent inhibitors against AchE with IC(50) values of 2.52 and 5.06 μM mL(−1). Additionally, 3d proved very good antimicrobial activity against all examined microorganisms with IZ (inhibition zone) over 25 mm and MIC (minimum inhibitory concentration) < 4 µM. Additionally, the ligand 2a and its corresponding ruthenium (II) complex 3a had good cytotoxic activity against both cancer cells HCT-116 and HepG-2, with IC(50) values of (7.76 and 11.76) and (4.12 and 9.21) μM mL(−1), respectively. Evaluation of the antiparasitic activity of these complexes against Leishmania major promastigotes and Toxoplasma gondii showed that ruthenium complexes were more potent than the free ligand, with an IC(50) values less than 1.5 μM mL(−1). However, 3d was found the best one with SI (selectivity index) values greater than 5 so it seems to be the best candidate for antileishmanial drug discovery program, and much future research are recommended for mode of action and in vivo evaluation. In general, Ru-NHC complexes are the most effective against L. major promastigotes. MDPI 2023-01-31 /pmc/articles/PMC9921063/ /pubmed/36771026 http://dx.doi.org/10.3390/molecules28031359 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Al Nasr, Ibrahim S. Koko, Waleed S. Khan, Tariq A. Gürbüz, Nevin Özdemir, Ismail Hamdi, Naceur Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title | Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title_full | Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title_fullStr | Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title_full_unstemmed | Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title_short | Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Enzymatic Inhibitory Agents with Antioxidant, Antimicrobial, Antiparasitical and Antiproliferative Activity |
title_sort | evaluation of ruthenium(ii) n-heterocyclic carbene complexes as enzymatic inhibitory agents with antioxidant, antimicrobial, antiparasitical and antiproliferative activity |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9921063/ https://www.ncbi.nlm.nih.gov/pubmed/36771026 http://dx.doi.org/10.3390/molecules28031359 |
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