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Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity

The synthesis, characterization, photophysical and biological properties of 13 new conjugate coumarin‐diruthenium(II)⋅arene complexes against Toxoplasma gondii are presented. For all conjugate organometallic unit/coumarins, an almost complete loss of fluorescence efficacy was observed. However, the...

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Autores principales: Desiatkina, Oksana, Păunescu, Emilia, Mösching, Martin, Anghel, Nicoleta, Boubaker, Ghalia, Amdouni, Yosra, Hemphill, Andrew, Furrer, Julien
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7586963/
https://www.ncbi.nlm.nih.gov/pubmed/32347622
http://dx.doi.org/10.1002/cbic.202000174
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author Desiatkina, Oksana
Păunescu, Emilia
Mösching, Martin
Anghel, Nicoleta
Boubaker, Ghalia
Amdouni, Yosra
Hemphill, Andrew
Furrer, Julien
author_facet Desiatkina, Oksana
Păunescu, Emilia
Mösching, Martin
Anghel, Nicoleta
Boubaker, Ghalia
Amdouni, Yosra
Hemphill, Andrew
Furrer, Julien
author_sort Desiatkina, Oksana
collection PubMed
description The synthesis, characterization, photophysical and biological properties of 13 new conjugate coumarin‐diruthenium(II)⋅arene complexes against Toxoplasma gondii are presented. For all conjugate organometallic unit/coumarins, an almost complete loss of fluorescence efficacy was observed. However, the nature of the fluorophore, the type of bonding, the presence and length of a linker between the coumarin dye and the ruthenium(II) moiety, and the number of dye units influenced their biological properties. The in vitro activity against a transgenic T. gondii strain grown in human foreskin fibroblasts (HFF) leads to IC(50) values for T. gondii β‐gal from 105 to 735 nM. Of note is that nine compounds displayed lower IC(50) than the standard drug pyrimethamine. One compound applied at its IC(50) did not affect B‐cell proliferation but had an impact on T‐cell proliferation in murine splenocyte cultures. Transmission electron microscopy of T. gondii β‐gal‐infected HFF showed that treatment predominantly affected the parasites’ mitochondrion.
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spelling pubmed-75869632020-10-30 Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity Desiatkina, Oksana Păunescu, Emilia Mösching, Martin Anghel, Nicoleta Boubaker, Ghalia Amdouni, Yosra Hemphill, Andrew Furrer, Julien Chembiochem Full Papers The synthesis, characterization, photophysical and biological properties of 13 new conjugate coumarin‐diruthenium(II)⋅arene complexes against Toxoplasma gondii are presented. For all conjugate organometallic unit/coumarins, an almost complete loss of fluorescence efficacy was observed. However, the nature of the fluorophore, the type of bonding, the presence and length of a linker between the coumarin dye and the ruthenium(II) moiety, and the number of dye units influenced their biological properties. The in vitro activity against a transgenic T. gondii strain grown in human foreskin fibroblasts (HFF) leads to IC(50) values for T. gondii β‐gal from 105 to 735 nM. Of note is that nine compounds displayed lower IC(50) than the standard drug pyrimethamine. One compound applied at its IC(50) did not affect B‐cell proliferation but had an impact on T‐cell proliferation in murine splenocyte cultures. Transmission electron microscopy of T. gondii β‐gal‐infected HFF showed that treatment predominantly affected the parasites’ mitochondrion. John Wiley and Sons Inc. 2020-06-16 2020-10-01 /pmc/articles/PMC7586963/ /pubmed/32347622 http://dx.doi.org/10.1002/cbic.202000174 Text en © 2020 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA This is an open access article under the terms of the http://creativecommons.org/licenses/by/4.0/ License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Full Papers
Desiatkina, Oksana
Păunescu, Emilia
Mösching, Martin
Anghel, Nicoleta
Boubaker, Ghalia
Amdouni, Yosra
Hemphill, Andrew
Furrer, Julien
Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title_full Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title_fullStr Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title_full_unstemmed Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title_short Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
title_sort coumarin‐tagged dinuclear trithiolato‐bridged ruthenium(ii)⋅arene complexes: photophysical properties and antiparasitic activity
topic Full Papers
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7586963/
https://www.ncbi.nlm.nih.gov/pubmed/32347622
http://dx.doi.org/10.1002/cbic.202000174
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