A new strategy for improving cytotoxicity of a copper complex toward metastatic melanoma cells unveiled by EPR spectroscopy.

A novel strategy of improving cytotoxicity against metastatic melanoma cells using an oxindolimine copper(ii) complex immobilized and dimerized on a modified Polyhedral Oligomeric Silsesquioxane (POSS) matrix was developed, as revealed by electron paramagnetic resonance (EPR) spectroscopy. An assured correlation between continuous-wave (CW) and pulsed EPR spectroscopies provided a complete characterization of the actual active species, its coordination environment, as well as the efficiency/selectivity of the bioconjugate materials.

Antitumor copper(II) complexes with hydroxyanthraquinones and N,N-heterocyclic ligands.

Five ternary copper(II) complexes, [Cu(phen)(L1)(ClO)] (1), [Cu(phen)(L1)(DMSO)](PF6) (2), [Cu(bpy)(L1)(ClO)(HO)] (3), [Cu(dmp)(L1)(ClO)(HO)] (4), and [Cu(phen)(L2)](ClO) (5), in which phen = 1,10-phenanthroline, bpy = 2,2'-bipyridine, dmp = 2,9-dimethyl-1,10-phenanthroline, HL1 = 1,4-dihydroxyanthracene-9,10-dione and HL2 = 1-hydroxyanthracene-9,10-dione, DMSO = dimethylsulfoxide, were synthesized and fully characterized. Complex 2 was obtained through the substitution of perchlorate for DMSO. When two hydroxyquinone groups are present, L1 makes a bridge between two Cu(II) ions, which also bind two nitrogens of the respective diimine ligand.

A bioinspired nitrone precursor to a stabilized nitroxide radical.

Nitrones derived from natural antioxidants are emerging as highly specific therapeutics against various human diseases, including stroke, neurodegenerative pathologies, and cancer. However, the development of useful pseudo-natural nitrones requires the judicious choice of a secondary metabolite as the precursor. Betalains are nitrogen-containing natural pigments that exhibit marked antioxidant capacity and pharmacological properties and, hence, are ideal candidates for designing multifunctional nitrones.

Unlike reactivity of mono- and binuclear imine-copper(II) complexes toward melanoma cells via a tyrosinase-dependent mechanism.

The cytotoxicity of a dinuclear imine-copper (II) complex 2, and its analogous mononuclear complex 1, toward different melanoma cells, particularly human SKMEL-05 and SKMEL-147, was investigated. Complex 2, a tyrosinase mimic, showed much higher activity in comparison to complex 1, and its reactivity was verified to be remarkably activated by UVB-light, while the mononuclear compound showed a small or negligible effect. Further, a significant dependence on the melanin content in the tumor cells, both from intrinsic pigmentation or stimulated by irradiation, was observed in the case of complex 2.