In continuation with our studies concerning the synthesis, characterization and biological evaluation of nucleolipidic Ru(III) complexes, a novel design for this family of potential anticancer agents is here presented. As a model compound, a new uridine-based nucleolipid has been prepared, named HoUrRu, following a simple and versatile synthetic procedure, and converted into a Ru(III) salt. Stable formulations of this highly functionalized Ru(III) complex have been obtained by co-aggregation with either the zwitterionic lipid POPC or the cationic DOTAP, which have been subjected to an in-depth microstructural characterization, including DLS, SANS and EPR measurements. The in vitro bioactivity profile of HoUrRu, as a pure compound or in formulation with POPC or DOTAP, reveals high antiproliferative activity on MCF-7 and WiDr human cancer cell lines.

A new design for nucleolipid-based Ru(III) complexes as anticancer agents

MONTESARCHIO, DANIELA;MANGIAPIA, GAETANO;VITIELLO, GIUSEPPE;MUSUMECI, DOMENICA;IRACE, CARLO;SANTAMARIA, RITA;D'ERRICO, GERARDINO;PADUANO, LUIGI
2013

Abstract

In continuation with our studies concerning the synthesis, characterization and biological evaluation of nucleolipidic Ru(III) complexes, a novel design for this family of potential anticancer agents is here presented. As a model compound, a new uridine-based nucleolipid has been prepared, named HoUrRu, following a simple and versatile synthetic procedure, and converted into a Ru(III) salt. Stable formulations of this highly functionalized Ru(III) complex have been obtained by co-aggregation with either the zwitterionic lipid POPC or the cationic DOTAP, which have been subjected to an in-depth microstructural characterization, including DLS, SANS and EPR measurements. The in vitro bioactivity profile of HoUrRu, as a pure compound or in formulation with POPC or DOTAP, reveals high antiproliferative activity on MCF-7 and WiDr human cancer cell lines.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11588/561987
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