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Ruthenium(III) complexes are very promising candidates as metal-based anticancer drugs, and several studies have supported the likely role of human serum proteins in the transport and selective delivery of Ru(III)-based compounds to tumor cells. Herein, the anticancer nanosystem composed of an amphiphilic nucleolipid incorporating a Ru(III) complex, which we named DoHuRu, embedded into the biocompatible cationic lipid DOTAP, was investigated as to its interaction with two human serum proteins thought to be involved in the mechanism of action of Ru(III)-based anticancer drugs, i.e., human serum albumin (HSA) and human transferrin (hTf). This nanosystem was studied in comparison with the simple Ru(III) complex named AziRu, a low molecular weight metal complex previously designed as an analogue of NAMI-A, decorated with the same ruthenium ligands as DoHuRu but devoid of the nucleolipid scaffold and not inserted in liposomal formulations. For this study, different spectroscopic techniques, i.e., Fluorescence Spectroscopy and Circular Dichroism (CD), were exploited, showing that DoHuRu/DOTAP liposomes can interact with both serum proteins without affecting their secondary structures. [ABSTRACT FROM AUTHOR]

A series of amorphous RuS2 and SBA-15 supported RuS2 materials were prepared by solvothermal method using corresponding tris-dialkyldithiocarbamato ruthenium(III) complexes as precursors. The structures of the catalystline precursors Ru(S2CNR2)3 (R = Me, Et, iPr), unsupported and supported amorphous RuS2-R materials as well as nanocrystalline RuS2 were characterized and analyzed by IR, powder X-ray diffraction (XRD), thermo-gravimetric analysis (TGA), transmission electron microscope (TEM), N2 sorption measurement, and temperature-programmed reduction (TPR). Powder X-ray diffraction patterns indicated the transformation of amorphous phase RuS2 to crystalline RuS2 with the heating treatment at 400 °C. The catalytic activity of RuS2-R/SBA-15 for thiophene hydrodesulfurization (HDS) was also investigated. [ABSTRACT FROM AUTHOR]

Ruthenium(III) complexes are very promising candidates as metal-based anticancer drugs, and several studies have supported the likely role of human serum proteins in the transport and selective delivery of Ru(III)-based compounds to tumor cells. Herein, the anticancer nanosystem composed of an amphiphilic nucleolipid incorporating a Ru(III) complex, which we named DoHuRu, embedded into the biocompatible cationic lipid DOTAP, was investigated as to its interaction with two human serum proteins thought to be involved in the mechanism of action of Ru(III)-based anticancer drugs, i.e., human serum albumin (HSA) and human transferrin (hTf). This nanosystem was studied in comparison with the simple Ru(III) complex named AziRu, a low molecular weight metal complex previously designed as an analogue of NAMI-A, decorated with the same ruthenium ligands as DoHuRu but devoid of the nucleolipid scaffold and not inserted in liposomal formulations. For this study, different spectroscopic techniques, i.e., Fluorescence Spectroscopy and Circular Dichroism (CD), were exploited, showing that DoHuRu/DOTAP liposomes can interact with both serum proteins without affecting their secondary structures.

New series of mononuclear octahedral Ru(III) complexes of general formula [RuL1-3Cl]Cl2 (1-3) where L = dianion of Schiff bases namely: 2,2'-(((1E,1'E)-thiophene-2,5-diylbis(methaneylylidene))bis(azaneylylidene))diphenol (H2L1), 2,2'-(((1E,1'E)-thiophene-2,5-diylbis(methaneylylidene))bis(azaneylylidene))dibenzenethiol (H2L2) and 2,2'-(((1E,1'E)-thiophene-2,5-diylbis(methaneylyli-dene))bis(azaneylyli-dene))-dibenzoic acid (H2L3), respectively are synthesized and characterized by different physico-chemical techniques. The results of interaction of complexes with CT-DNA supported that, the Ru (III) complexes bind to DNA via an intercalative mode. The interaction has also been investigated by gel electrophoresis. Interestingly, it was found that all Ru(III) complexes cleave super coiled (SC) pUC19 plasmid DNA efficiently in the absence of an external agent. Further, the antiproliferative activity of the complexes on Human Cervical Cancer Cells (HeLa) and Human Breast Cancer Cells (MCF-7) were evaluated by MTT assay, which revealed that, all the complexes showed more intense inhibition against HeLa and MCF-7 cell lines, particularly Ru(III) complex (3) attenuated the strongest proliferation, allowing its use as chemotherapeutic agent for cancer treatment.

This study evaluates the genotoxic potential of two Ru(III) complexes with thiosemicarbazone based ligands. The complexes were tested for in vitro protective effect on chromosome aberrations in peripheral human lymphocytes using the cytokinesis block micronucleus (CBMN) assay at concentrations 1.5; 3.7 and 7.4 μg/mL. The cell culture treated with the tested complexes, at 3.7 μg/mL concentration, decreased a frequency of micronucleus for 37% and 32%, when compared with the control cell cultures. At concentration of 7.4 (1.5) μg/mL of this complexes exhibited slightly lower effect of micronucleus for 30% (35%) and 27% (29%), when compared with the control cell cultures. [ABSTRACT FROM AUTHOR]

In our search for new anticancer and DNA interacting agents, ruthenium(III) thiosemicarbazone complexes of the type [RuCl2(EPh3)L] (where E = P/As; L = monobasic tridentate thiosemicarbazone ligand) were synthesized and characterized by physico-chemical and spectroscopic methods. All the ligands and complexes exhibit noticeable growth inhibition against fungal species and bacterial species. The interactions of these complexes with biomolecule, CT-DNA were investigated by absorbance measurement and gel electrophoresis. Absorption spectral study indicates that the ruthenium(III) complexes have an intrinsic binding constant in the range of 1.0–3.6 × 104 M−1. The complexes exhibit a remarkable DNA cleavage activity with CT-DNA in the presence of hydroxyl radical. The cleavage activity was carried out with the variation of the concentration of complexes and incubation time. Further, an in vitro cytotoxicity study of the complexes exhibited antitumor activity against the HeLa tumor cell line. This research may provide valuable insight into the interactions of metal complexes with DNA and cytotoxicity, knowledge that is an excellent back drop for the rational design of promising drugs.

The great advances in the studies on metal complexes for the treatment of different cancer forms, starting from the pioneering works on platinum derivatives, have fostered an increasingly growing interest in their properties and biomedical applications. Among the various metal-containing drugs investigated thus far, ruthenium(III) complexes have emerged for their selective cytotoxic activity in vitro and promising anticancer properties in vivo, also leading to a few candidates in advanced clinical trials. Aiming at addressing the solubility, stability and cellular uptake issues of low molecular weight Ru(III)-based compounds, some research groups have proposed the development of suitable drug delivery systems (e.g., taking advantage of nanoparticles, liposomes, etc.) able to enhance their activity compared to the naked drugs. This review highlights the unique role of Ru(III) complexes in the current panorama of anticancer agents, with particular emphasis on Ru-containing nanoformulations based on the incorporation of the Ru(III) complexes into suitable nanocarriers in order to enhance their bioavailability and pharmacokinetic properties. Preclinical evaluation of these nanoaggregates is discussed with a special focus on the investigation of their mechanism of action at a molecular level, highlighting their pharmacological potential in tumour disease models and value for biomedical applications.

Ruthenium(III) complexes of the type [RuX2(PPh3)(L)] (where X = Cl/Br; L = Benzothiazolyl-Salal Schiff base ligand) has been synthesized. The synthesized complexes were characterized by various physicochemical and spectral techniques. An octahedral geometry has been tentatively proposed for all the complexes. The cytotoxic activity of the synthesized ruthenium(III) complexes has shown significant activity against a panel of microbes. [ABSTRACT FROM AUTHOR]

Abstract: A redox active self-assembled monolayer consisting of ethylenediamine moieties coordinated to RuIII ions was prepared through a vapor phase silane coupling of N-(2-aminoethyl)-3-aminopropyltrimethoxysilane (AEAPS) molecules onto a SiO2/Si substrate, followed by complexation of RuIII ions in an aqueous RuCl3 solution. A similar SAM with 3-aminopropyltriethoxysilane did not provide surface RuIII-complex, indicating that chelation ability plays a key role in immobilizing RuIII ions at the surface. The RuIII chelated AEAPS-SAM gave a couple of RuIII/RuIV redox peaks at +1.0 and −0.1V vs. Ag/AgCl (3moldm−3 NaCl). [Copyright &y& Elsevier]

The great advances in the studies on metal complexes for the treatment of different cancer forms, starting from the pioneering works on platinum derivatives, have fostered an increasingly growing interest in their properties and biomedical applications. Among the various metal-containing drugs investigated thus far, ruthenium(III) complexes have emerged for their selective cytotoxic activity in vitro and promising anticancer properties in vivo, also leading to a few candidates in advanced clinical trials. Aiming at addressing the solubility, stability and cellular uptake issues of low molecular weight Ru(III)-based compounds, some research groups have proposed the development of suitable drug delivery systems (e.g., taking advantage of nanoparticles, liposomes, etc.) able to enhance their activity compared to the naked drugs. This review highlights the unique role of Ru(III) complexes in the current panorama of anticancer agents, with particular emphasis on Ru-containing nanoformulations based on the incorporation of the Ru(III) complexes into suitable nanocarriers in order to enhance their bioavailability and pharmacokinetic properties. Preclinical evaluation of these nanoaggregates is discussed with a special focus on the investigation of their mechanism of action at a molecular level, highlighting their pharmacological potential in tumour disease models and value for biomedical applications. [ABSTRACT FROM AUTHOR]

In our search for new anticancer and DNA interacting agents, ruthenium(III) thiosemicarbazone complexes of the type [RuCl 2 (EPh 3 )L] (where E = P/As; L = monobasic tridentate thiosemicarbazone ligand) were synthesized and characterized by physico-chemical and spectroscopic methods. All the ligands and complexes exhibit noticeable growth inhibition against fungal species and bacterial species. The interactions of these complexes with biomolecule, CT-DNA were investigated by absorbance measurement and gel electrophoresis. Absorption spectral study indicates that the ruthenium(III) complexes have an intrinsic binding constant in the range of 1.0–3.6 × 10 4 M −1 . The complexes exhibit a remarkable DNA cleavage activity with CT-DNA in the presence of hydroxyl radical. The cleavage activity was carried out with the variation of the concentration of complexes and incubation time. Further, an in vitro cytotoxicity study of the complexes exhibited antitumor activity against the HeLa tumor cell line. This research may provide valuable insight into the interactions of metal complexes with DNA and cytotoxicity, knowledge that is an excellent back drop for the rational design of promising drugs. [ABSTRACT FROM AUTHOR]