Coumarin-Tagged Dinuclear Trithiolato-Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity |
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Authors: | Oksana Desiatkina Emilia Păunescu Martin Mösching Nicoleta Anghel Ghalia Boubaker Yosra Amdouni Andrew Hemphill Dr Julien Furrer |
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Affiliation: | 1. Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, 3012 Bern, Switzerland;2. Institute of Parasitology Vetsuisse Faculty, University of Bern, Länggass-Strasse 122, 3012 Bern, Switzerland |
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Abstract: | 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 IC50 values for T. gondii β-gal from 105 to 735 nM. Of note is that nine compounds displayed lower IC50 than the standard drug pyrimethamine. One compound applied at its IC50 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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Keywords: | antiprotozoal agents coumarin cytotoxicity ruthenium sandwich complexes Toxoplasma gondii |
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