Coumarin-Tagged Dinuclear Trithiolato-Bridged Ruthenium(II)?Arene Complexes: Photophysical Properties and Antiparasitic Activity.

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 ?-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 ?-gal-infected HFF showed that treatment predominantly affected the parasites' mitochondrion.

SUBMITTER: Desiatkina O 

PROVIDER: S-EPMC7586963 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature