Continuing the study of the physico-chemical and biological properties of ruthenium-quinolone adducts, four novel complexes with the general formula [Ru([9]aneS3)(dmso-κS)(quinolonato-κ2O,O)](PF6), containing the quinolones levofloxacin (1), nalidixic acid (2), oxolinic acid (3), and cinoxacin (4), were prepared and characterized in solid state as well as in solution. Contrary to their organoruthenium analogues, these complexes are generally relatively stable in aqueous solution as substitution of the dmso ligand is slow and not quantitative, and a minor release of the quinolonato ligand is observed only in the case of 4. The complexes bind to serum proteins displaying relatively high binding constants. DNA binding was studied using UV-Vis spectroscopy, cyclic voltammetry and performing viscosity measurements of CT DNA solutions in the presence of complexes 1–4. These experiments show that the ruthenium complexes interact with DNA via intercalation. Compounds 2 and 4 exhibit a weak inhibition of cathepsins B and S, which are involved in the progression of a number of diseases, including cancer. Furthermore, complexes displayed moderate cytotoxicity when tested on the HeLa cell line.
COBISS.SI-ID: 1610287
In addition to quinolones, which are typical O,O ligands, we have also decided to prepare ruthenium complexes of various ß-diketonates. Such ligands coordinate similarly as quinolones and it is known that their metal complexes exert interesting physico-chemical and biological properties. Five different fluorinated β-diketone ligands in the presence of sodium methoxide easily react with the organoruthenium precursor generating neutral complexes 1–5 with typical ‘‘piano-stool’’ geometry. All synthesized compounds were characterized by multinuclear NMR, X-ray diffraction and other standard physico-chemical methods. It was found that these compounds are ready-to-use catalysts, which are efficient for direct arylation of 2-phenylpyridine. Literature data revealed that frequently, compounds with catalytic properties exert also biological activity and we plan to test biological activity of isolated compounds in the future.
COBISS.SI-ID: 36426757
Conjoint liquid chromatography (CLC) on monolithic convective interaction media (CIM) disks coupled on-line to UV and inductively coupled plasma mass spectrometry (ICP-MS) detectors was used in speciation analysis of Pt in human serum spiked with Pt-based chemotherapeutics. CIM Protein G and CIM DEAE disks were assembled together in a single housing forming a CLC monolithic column. Such a set-up allows rapid two-dimensional separation by affinity and ion-exchange (IE) modes to be carried out in a single chromatographic run. Separated Pt species were quantified by post-column isotope dilution—ICP-MS. The method developed may be reliably applied in preclinical and clinical studies of the kinetics of the interaction and distribution of different metallodrugs with proteins in blood serum.
COBISS.SI-ID: 26734631