title: Cholesterol-based nucleolipid-ruthenium complex stabilized by lipid aggregates for antineoplastic therapy.
abstract: A novel ruthenium complex, linked to a cholesterol-containing nucleolipid (named ToThyCholRu), stabilized by lipid aggregates for antineoplastic therapy is presented. In order to retard the degradation kinetics typically observed for several ruthenium-based antineoplastic agents, ToThyCholRu is incorporated into a liposome bilayer formed by POPC. The resulting nanoaggregates contain up to 15% in moles of the ruthenium complex, and are shown to be stable for several weeks. The liposomes host the ruthenium-nucleolipid complex with the metal ion surrounded by POPC lipid headgroups and the steroid moiety inserted in the more external acyl chain region. These ruthenium-containing liposomes are more effective in inhibiting the growth of cancer cells than a model NAMI-A-like ruthenium complex, prepared for a direct evaluation of their anti-proliferative activity. These results introduce new perspectives in the design of innovative transition-metal-based supramolecular systems for anticancer drug vectorization.
authors.affiliation: Dipartimento di Chimica Organica e Biochimica, Università Federico II di Napoli, Complesso Universitario di Monte S. Angelo, via Cintia, 4, 80126 Naples, Italy.
authors.forename: Luca
authors.initials: L
authors.lastname: Simeone
authors.forename: Gaetano
authors.initials: G
authors.lastname: Mangiapia
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Vitiello
authors.forename: Carlo
authors.initials: C
authors.lastname: Irace
authors.forename: Alfredo
authors.initials: A
authors.lastname: Colonna
authors.forename: Ornella
authors.initials: O
authors.lastname: Ortona
authors.forename: Daniela
authors.initials: D
authors.lastname: Montesarchio
authors.forename: Luigi
authors.initials: L
authors.lastname: Paduano
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002784:Cholesterol / Q000737:chemistry*; D004355:Drug Stability; D006801:Humans; D033363:Neutron Diffraction; D009942:Organometallic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*; D053838:Scattering, Small Angle
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D012428:Ruthenium; D002784:Cholesterol