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Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin
Metal complexes displaying antiplatelet properties is a promising research area. In our methodology, Platelet-Activating Factor (PAF), the most potent lipid pro-inflammatory mediator, serves as a biological probe. The antiplatelet activity is exerted by the inhibition of the PAF-induced aggregation...
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/PMC9964123/ https://www.ncbi.nlm.nih.gov/pubmed/36838847 http://dx.doi.org/10.3390/molecules28041859 |
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author | Kalampalidis, Alexandros Damati, Artemis Matthopoulos, Demetrios Tsoupras, Alexandros B. Demopoulos, Constantinos A. Schnakenburg, Gregor Philippopoulos, Athanassios I. |
author_facet | Kalampalidis, Alexandros Damati, Artemis Matthopoulos, Demetrios Tsoupras, Alexandros B. Demopoulos, Constantinos A. Schnakenburg, Gregor Philippopoulos, Athanassios I. |
author_sort | Kalampalidis, Alexandros |
collection | PubMed |
description | Metal complexes displaying antiplatelet properties is a promising research area. In our methodology, Platelet-Activating Factor (PAF), the most potent lipid pro-inflammatory mediator, serves as a biological probe. The antiplatelet activity is exerted by the inhibition of the PAF-induced aggregation in washed rabbit platelets (WRPs) and in rabbit plasma rich in platelets (rPRPs). Herein, the synthesis and biological investigation of a series of organometallic tin(II) and tin(IV) complexes, featuring the oxygen tripodal Kläui ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), {R = H, (L(OEt)(−)); Me (L*(OEt)(−))}, are reported. Reaction of NaL(OEt) (1a) and NaL*(OEt) (1b) with SnCl(2), yielded the rare four-coordinate L(OEt)SnCl (2a) and L*(OEt)SnCl (2b) complexes. Accordingly, L(OEt)SnPh(3) (3a) and L*(OEt)SnPh(3) (3b) were prepared, starting from Ph(3)SnCl. Characterization includes spectroscopy and X-ray diffraction studies for 2a, 2b and 3b. The antiplatelet activity of the lead complexes 2b and 3a (IC(50) = 0.5 μΜ) is superior compared to that of 1a and 1b, while both complexes display a pronounced inhibitory activity against thrombin (IC(50) = 1.8 μM and 0.6 μM). The in vitro cytotoxic activities of 3a and 2b on human Jurkat T lymphoblastic tumor cell line is higher than that of cisplatin. |
format | Online Article Text |
id | pubmed-9964123 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-99641232023-02-26 Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin Kalampalidis, Alexandros Damati, Artemis Matthopoulos, Demetrios Tsoupras, Alexandros B. Demopoulos, Constantinos A. Schnakenburg, Gregor Philippopoulos, Athanassios I. Molecules Article Metal complexes displaying antiplatelet properties is a promising research area. In our methodology, Platelet-Activating Factor (PAF), the most potent lipid pro-inflammatory mediator, serves as a biological probe. The antiplatelet activity is exerted by the inhibition of the PAF-induced aggregation in washed rabbit platelets (WRPs) and in rabbit plasma rich in platelets (rPRPs). Herein, the synthesis and biological investigation of a series of organometallic tin(II) and tin(IV) complexes, featuring the oxygen tripodal Kläui ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), {R = H, (L(OEt)(−)); Me (L*(OEt)(−))}, are reported. Reaction of NaL(OEt) (1a) and NaL*(OEt) (1b) with SnCl(2), yielded the rare four-coordinate L(OEt)SnCl (2a) and L*(OEt)SnCl (2b) complexes. Accordingly, L(OEt)SnPh(3) (3a) and L*(OEt)SnPh(3) (3b) were prepared, starting from Ph(3)SnCl. Characterization includes spectroscopy and X-ray diffraction studies for 2a, 2b and 3b. The antiplatelet activity of the lead complexes 2b and 3a (IC(50) = 0.5 μΜ) is superior compared to that of 1a and 1b, while both complexes display a pronounced inhibitory activity against thrombin (IC(50) = 1.8 μM and 0.6 μM). The in vitro cytotoxic activities of 3a and 2b on human Jurkat T lymphoblastic tumor cell line is higher than that of cisplatin. MDPI 2023-02-16 /pmc/articles/PMC9964123/ /pubmed/36838847 http://dx.doi.org/10.3390/molecules28041859 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 Kalampalidis, Alexandros Damati, Artemis Matthopoulos, Demetrios Tsoupras, Alexandros B. Demopoulos, Constantinos A. Schnakenburg, Gregor Philippopoulos, Athanassios I. Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title | Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title_full | Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title_fullStr | Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title_full_unstemmed | Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title_short | Tin(II) and Tin(IV) Complexes Incorporating the Oxygen Tripodal Ligands [(η(5)-C(5)R(5))Co{P(OEt)(2)O}(3)](−), (R = H, Me; Et = -C(2)H(5)) as Potent Inflammatory Mediator Inhibitors: Cytotoxic Properties and Biological Activities against the Platelet-Activating Factor (PAF) and Thrombin |
title_sort | tin(ii) and tin(iv) complexes incorporating the oxygen tripodal ligands [(η(5)-c(5)r(5))co{p(oet)(2)o}(3)](−), (r = h, me; et = -c(2)h(5)) as potent inflammatory mediator inhibitors: cytotoxic properties and biological activities against the platelet-activating factor (paf) and thrombin |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9964123/ https://www.ncbi.nlm.nih.gov/pubmed/36838847 http://dx.doi.org/10.3390/molecules28041859 |
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