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Journal of Inorganic Biochemistry
Elsevier Science Publishing Co.
Journal of Inorganic Biochemistry

Elsevier Science Publishing Co.

0162-0134

Journal of Inorganic Biochemistry/Journal Journal of Inorganic BiochemistrySCIISTPAHCI
正式出版
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    Zinc ionophores: chemistry and biological applications

    Scavo, SimoneOliveri, Valentina
    11页
    查看更多>>摘要:Zinc can play a pathophysiological role in several diseases and can interfere in key processes of microbial growth. This evidence justifies the efforts in applying Zinc ionophores to restore Zinc homeostasis and treat bacterial/ viral infections such as coronavirus diseases. Zinc ionophores increase the intracellular concentration of Zinc ions causing significant biological effects. This review provides, for the first time, an overview of the applications of the main Zinc ionophores in Zinc deficiency, infectious diseases, and in cancer, discussing the pharmacological and coordination properties of the Zinc ionophores.

    In vitro biological activity of copper(II) complexes with NSAIDs and nicotinamide: characterization, DNA- and BSA-interaction study and anticancer activity

    Jozefikova, FloraPerontsis, SpyrosMoncol, JanMazur, Milan...
    14页
    查看更多>>摘要:Through the reaction of copper(II) acetate with nicotinamide (pyridine-3-carboxylic acid amide, niacinamide) and some derivatives of N-phenylanthranilic acid (fenamates), seven new mixed-ligand copper(II) compounds were isolated: [Cu(tolf-O)(tolf-O,O')nia-N)(2)(EtOH)] (1), [Cu(tolf-O)(tolf-O,O')(nia-N)(2)(MeOH)] (2), [Cu(meclfO)(meclf-O,O')(nia-N)(2)(EtOH)] (3), [Cu(meclf-O)(meclf-O,O')(nia-N)(2)(MeOH)] (4), [Cu(meclf-O)(meclf-O,O') (nia-N)(2)(ACN)] (5), [Cu(mef-O)(mef-O,O')(nia-N)(2)(EtOH)] (6) and [Cu(mef-O)(mef-O,O')(nia-N)(2)(ACN)] (7) containing a molecule of relevant solvent as ligand in their primary crystal structure (tolf = tolfenamate, meclf = meclofenamate, mef = mefenamate, nia = nicotinamide, EtOH = ethanol, MeOH = methanol, ACN = acetonitrile). The structures of the complexes were determined by single-crystal X-ray analysis. The intermolecular interactions were studied by Hirshfeld surface analysis. The complexes were characterized by IR, UV-vis and EPR spectroscopy and their redox properties were determined by cyclic voltammetry. The interaction of the complexes with bovine serum albumin was studied by fluorescence emission spectroscopy and the albumin-binding constants of the compounds were calculated. The interaction of the complexes with calf-thymus DNA was monitored by diverse techniques (UV-vis spectroscopy, cyclic voltammetry, viscosity measurements) suggesting intercalation as the most possible mode of binding. DNA-competitive studies of the complexes with ethidium bromide were monitored by fluorescence emission spectroscopy. The cytotoxic effects of copper(II) complexes on lung carcinoma cells and healthy cells were determined by the MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] colorimetric technique.

    Biocompatible silver(I) complexes with heterocyclic thioamide ligands for selective killing of cancer cells and high antimicrobial activity-A combined in vitro and in silico study

    Varna, DespoinaGeromichalou, ElenaPapachristou, EleniPapi, Rigini...
    18页
    查看更多>>摘要:A series of heteroleptic Ag(I) complexes bearing 4,6-dimethyl-2-pyrimidinethiol (dmp2SH), i.e., [AgCl(dmp2SH) (PPh3)(2)] (1), [Ag(dmp2SH)(PPh3)(2)]NO3 (2), [Ag(dmp2SH)(xantphos)]NO3 (3), [Ag(mu-dmp2S)(PPh3)](2) (4), [Ag (dmp2S)(xantphos)] (5), [Ag(mu-dmp2S)(DPEphos)]2 (6) (xantphos = 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene and DPEPhos = bis[(2-diphenylphosphino)phenyl]ether) were synthesized. The complexes display systematic variation of particular structural characteristics which were proved to have a significant impact on their in vitro cytotoxicity and antimicrobial properties. A moderate-to-high potential for bacteria growth inhibition was observed for all complexes, with 2, 3 and 5 being particularly effective against Gram-(+) bacteria (IC50 = 1.6-4.5 mu M). The three complexes exhibit high in vitro cytotoxicity against HeLa and MCF-7 cancer cells (IC50 = 0.32-3.00 mu\M), suggesting the importance of coordination unsaturation and cationic charge for effective bioactivity. A very low cytotoxicity against HDFa normal cells was observed, revealing a high degree of selectivity (selectivity index similar to 10) and, hence, biocompatibility. Fluorescence microscopy using 2 showed effective targeting on the membrane of the HeLa cancer cells, subsequently inducing cell death. Binding of the complexes to serum albumin proteins is reasonably strong for potential uptake and subsequent release to target sites. A moderate in vitro antioxidant capacity for free radicals scavenging was observed and a low potential to destroy the double-strand structure of calf-thymus DNA by intercalation, suggesting likely implication of these properties in the bioactivity mechanisms of these complexes. Further insight into possible mechanisms of bioactivity was obtained by molecular modeling calculations, by exploring their ability to act as potential inhibitors of DNAgyrase, human estrogen receptor alpha, human cyclin-dependent kinase 6, and human papillomavirus E6 oncoprotein.