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Highly Charged Ruthenium(II) Polypyridyl Complexes as Effective Photosensitizer in Photodynamic Therapy
Authors:Dr Luca Conti  Prof Andrea Bencini  Prof Camilla Ferrante  Dr Cristina Gellini  Prof Paolo Paoli  Dr Matteo Parri  Prof Giangaetano Pietraperzia  Prof Barbara Valtancoli  Prof Claudia Giorgi
Institution:1. Department of Chemistry ‘Ugo Schiff', University of Florence, Via della Lastruccia 3, 50019 Sesto Fiorentino (FI), Italy;2. Department of Chemical Sciences and UR INSTM, University of Padova, via Marzolo 1, 35131 Padova (PD), Italy;3. Department of Experimental and Clinical Biomedical Sciences “Mario Serio”, University of Florence, Viale Morgagni 50, Firenze (FI), Italy;4. Department of Chemistry ‘Ugo Schiff', University of Florence, Via della Lastruccia 3, 50019 Sesto Fiorentino (FI), Italy

European Laboratory for Non Linear Spectroscopy (LENS), University of Florence, via Nello Carrara 1, 50019 Sesto Fiorentino (FI), Italy

Abstract:A comparative study between two novel, highly water soluble, ruthenium(II) polypyridyl complexes, Ru(phen)2 L ′] and Ru(phen)2Cu(II) L ′] ( L and L -CuII), containing the polyaazamacrocyclic unit 4,4′-(2,5,8,11,14-pentaaza15])-2,2′-bipyridilophane ( L ′), is herein reported. L and L -CuII interact with calf-thymus DNA and efficiently cleave DNA plasmid when light-activated. They also possess great penetration abilities and photo-induced biological activities, evaluated on an A375 human melanoma cell line, with L -CuII being the most effective. Our study highlights the key role of the Fenton active CuII center within the macrocycle framework, that would play a synergistic role with light activation in the formation of cytotoxic ROS species. Based on these results, an optimal design of RuII polypyridyl systems featuring specific CuII-chelating polyamine units could represent a suitable strategy for the development of novel and effective photosensitizers in photodynamic therapy.
Keywords:Photodynamic Therapy  Polypyridyl ligands  ROS  Ruthenium(II) complexes
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