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Your search keyword '"Massai, Lara"' showing total 12 results
Start Over Author "Massai, Lara" Journal biometals
12 results on '"Massai, Lara"'

7. New platinum(II) and palladium(II) complexes with substituted terpyridine ligands: synthesis and characterization, cytotoxicity and reactivity towards biomolecules.

Author

Savić, Aleksandar, Marzo, Tiziano, Scaletti, Federica, Massai, Lara, Bartoli, Gianluca, Hoogenboom, Richard, Messori, Luigi, Van Deun, Rik, and Van Hecke, Kristof

Abstract

A series of palladium(II) (1-3) and platinum(II) chloride complexes (4 and 5) with 2,2′:6′,2″-terpyridine (terpy) derivatives substituted at the 4′ position, was synthesized and fully characterized. Single crystal X-ray diffraction analysis of complexes 2, 3 and 5 showed tridentate coordination of the 4′-substituted terpyridine (terpy) ligands to the metal center. Moreover, in vitro cytotoxic activity of these complexes toward a panel of human cancer cell lines (lung cancer A549, colorectal cancer HCT116, ovarian cancer IGROV-1) and toward normal cell line HDF (dermal fibroblast) was determined by Trypan Blue exclusion assay. Overall, the tested compounds manifested a relevant cytotoxicity for the selected cancer cell lines with complex 4 also showing a modest cytotoxicity on the normal cell lines. To better understand the mode of action of these metal complexes, their reactivity with three model proteins, i.e. hen egg white lysozyme (HEWL), cytochrome c (cyt c) and ribonuclease A (RNase A) were comparatively investigated through ESI-MS analysis. The results highlighted a different behavior between the two series of complexes being platinum compounds more reactive toward RNase and cyt c than palladium compounds. Based on the obtained results, it is proposed that in presence of RNase A and cyt c, the platinum complexes undergo activation through release of labile ligands followed by binding to the protein. In contrast, palladium complexes revealed a far lower reactivity implying the likely occurrence of a different mechanism of action. [ABSTRACT FROM AUTHOR]

Published
2019
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9. Reactions of cytotoxic metallodrugs with lysozyme in pure DMSO explored through UV-Vis absorption spectroscopy and ESI MS

Author

Marzo, Tiziano, Savić, Aleksandar, Massai, Lara, Michelucci, Elena, Sabo, Tibor, Grgurić-Šipka, Sanja, Messori, Luigi, Marzo, Tiziano, Savić, Aleksandar, Massai, Lara, Michelucci, Elena, Sabo, Tibor, Grgurić-Šipka, Sanja, and Messori, Luigi

Abstract

The reactions of four representative metallodrugs with the model protein HEWL were investigated within a non-aqueous environment-i.e. in pure DMSO- through UV-Vis absorption spectroscopy and ESI MS analysis. Notably, formation of a variety of metallodrug-protein adducts was clearly documented. This is the first example for this kind of protein metalation reactions carried out within a pure organic solvent. It is shown that the applied solution conditions greatly affect the nature of the formed adducts, this being well accounted for by the fact that the overall protein conformation is greatly perturbed within pure DMSO; in addition, the activation profiles of the studied metallodrugs are also highly dependent on the nature of the solvent. The implications of these results are discussed.

Published
2015

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