Back to Search
Start Over
Coumarin‐Tagged Dinuclear Trithiolato‐Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity
- Source :
- Chembiochem, Desiatkina, Oksana; Păunescu, Emilia; Mösching, Martin; Anghel, Nicoleta; Boubaker, Ghalia; Amdouni, Yosra; Hemphill, Andrew; Furrer, Julien (2020). Coumarin-Tagged Dinuclear Trithiolato-Bridged Ruthenium(II)⋅Arene Complexes: Photophysical Properties and Antiparasitic Activity. ChemBioChem, 21(19), pp. 2818-2835. Wiley-VCH 10.1002/cbic.202000174
- Publication Year :
- 2020
- Publisher :
- Wiley, 2020.
-
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.<br />The (para)site for treatment: Thirteen coumarin‐diruthenium(II)⋅arene conjugates were evaluated against a transgenic T. gondii strain grown in human foreskin fibroblasts (HFF). The IC50 values ranged from 105 to 735 nM, with nine compounds displaying a lower IC50 than the standard drug pyrimethamine. TEM of T. gondii‐infected HFF showed that treatment predominantly affected the parasites’ mitochondrion.
- Subjects :
- Models, Molecular
Crystallography, X-Ray
coumarin
01 natural sciences
Biochemistry
Mice
chemistry.chemical_compound
Parasitic Sensitivity Tests
Coordination Complexes
Coumarins
540 Chemistry
Moiety
Cells, Cultured
Mice, Inbred BALB C
Antiparasitic Agents
Molecular Structure
Full Paper
630 Agriculture
biology
Full Papers
Photochemical Processes
Fluorescence
Ruthenium
cytotoxicity
Molecular Medicine
Female
Toxoplasma
antiprotozoal agents
Fluorophore
Stereochemistry
sandwich complexes
Toxoplasma gondii
chemistry.chemical_element
010402 general chemistry
parasitic diseases
Animals
Humans
Sulfhydryl Compounds
Molecular Biology
Cell Proliferation
010405 organic chemistry
Organic Chemistry
biology.organism_classification
Coumarin
0104 chemical sciences
chemistry
570 Life sciences
Linker
Conjugate
Subjects
Details
- ISSN :
- 14397633 and 14394227
- Volume :
- 21
- Database :
- OpenAIRE
- Journal :
- ChemBioChem
- Accession number :
- edsair.doi.dedup.....0ed595cee9641cf3254838d588f7cca6