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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...

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Detalles Bibliográficos
Autores principales: Kalampalidis, Alexandros, Damati, Artemis, Matthopoulos, Demetrios, Tsoupras, Alexandros B., Demopoulos, Constantinos A., Schnakenburg, Gregor, Philippopoulos, Athanassios I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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.
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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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