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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...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
John Wiley and Sons Inc.
2020
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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. |
format | Online Article Text |
id | pubmed-7586963 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
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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