👤 Chen MR

Four ruthenium(II)-based complexes with N-(acyl)-N',N'-(disubstituted)thiourea derivatives (Th) were obtained. The compounds, with the general formula trans-[Ru(PPh3)2(Th)(bipy)]PF6, interact with bovine serum albumin (BSA) and DNA. BSA-binding constants, which were in the range of 3.3-6.5×10(4) M(-1), and the thermodynamic parameters (ΔG, ΔH and ΔS), suggest spontaneous interactions with this protein by electrostatic forces due to the positive charge of the complexes. Also, binding constant by spectrophotometric DNA titration (Kb = 0.8-1.8×10(4) M(-1)) and viscosity studies indicate weak interactions between the complexes and DNA. Cytotoxicity assays against DU-145 (prostate cancer) and A549 (lung cancer) tumour cells revealed that the complexes are more active in tumour cells than in normal (L929) cells, and that they present high cytotoxicity (low IC50 values) compared with the reference metallodrug, cisplatin. Show less

The novel ligand (dmbip) 2-(4-N, N-dimethylbenzenamine)1H-imidazo[4, 5-f][1, 10]phenanthroline and its complexes [Ru(phen)2dmbip](2+) (1), [Ru(bpy)2dmbip](2+) (2), [Co(phen)2dmbip](3+) (3) and [Co(bpy)2dmbip](3+) (4) [where phen = 1, 10-phenanthroline, bpy = 2, 2'-bipyridine], have been synthesized and characterized by elemental analysis, IR, UV-Vis, (1)H NMR, (13)C NMR and Mass spectra. The DNA binding properties of the complexes were investigated by absorption, emission, quenching studies, light switch "on and off", salt dependent, sensor (cation and anion) studies, viscosity measurements, cyclic voltammetry, molecular modeling and docking studies. The four complexes were screened for Photo cleavage of pBR322 DNA, antimicrobial activity and cytotoxicity. The experimental results indicate that the four complexes can intercalate into DNA base pairs. The DNA-binding affinities of these complexes follow the order [Ru(phen)2dmbip](2+) > [Co(phen)2dmbip](3+) > [Ru(bpy)2dmbip](2+) > [Co(bpy)2dmbip](3+). Show less

The monodentate cis-[Ru(phen)(2)(hist)(2)](2+)1R and the bidentate cis-[Ru(phen)(2)(hist)](2+)2A complexes were prepared and characterized using spectroscopic ((1)H, ((1)H-(1)H)COSY and ((1)H-(13)C)HSQC NMR, UV-vis, luminescence) techniques. The complexes presented absorption and emission in the visible region, as well as a tri-exponential emission decay. The complexes are soluble in aqueous and non-aqueous solution with solubility in a buffer solution of pH 7.4 of 1.14 × 10(-3) mol L(-1) for (1R + 2A) and 6.43 × 10(-4) mol L(-1) for 2A and lipophilicity measured in an aqueous-octanol solution of -1.14 and -0.96, respectively. Photolysis in the visible region in CH(3)CN converted the starting complexes into cis-[Ru(phen)(2)(CH(3)CN)(2)](2+). Histamine photorelease was also observed in pure water and in the presence of BSA (1.0 × 10(-6) mol L(-1)). The bidentate coordination of the histamine to the ruthenium center in relation to the monodentate coordination increased the photosubstitution quantum yield by a factor of 3. Pharmacological studies showed that the complexes present a moderate inhibition of AChE with an IC(50) of 21 μmol L(-1) (referred to risvagtini, IC(50) 181 μmol L(-1) and galantamine IC(50) 0.006 μmol L(-1)) with no appreciable cytotoxicity toward to the HeLa cells (50% cell viability at 925 μmol L(-1)). Cell uptake of the complexes into HeLa cells was detected by fluorescence confocal microscopy. Overall, the observation of a luminescent complex that penetrates the cell wall and has low cytotoxicity, but is reactive photochemically, releasing histamine when irradiated with visible light, are interesting features for application of these complexes as phototherapeutic agents. Show less