title: Biological activity and cellular uptake of [Ru(η5-C5H5)(PPh3)(Me2bpy)][CF3SO3] complex.
abstract: Anticancer activity of the new [Ru(η(5)-C5H5)(PPh3)(Me2bpy)][CF3SO3] (Me2bpy = 4,4'-dimethyl-2,2'-bipyridine) complex was evaluated in vitro against several human cancer cell lines, namely A2780, A2780CisR, HT29, MCF7, MDAMB231 and PC3. Remarkably, the IC50 values, placed in the nanomolar and sub-micromolar range, largely exceeded the activity of cisplatin. Binding to human serum albumin, either HSA (human serum albumin) or HSA(faf) (fatty acid-free human serum albumin) does not affect the complex activity. Fluorescence studies revealed that the present ruthenium complex strongly quench the intrinsic fluorescence of albumin. Cell death by the [Ru(η(5)-C5H5)(PPh3)(Me2bpy)][CF3SO3] complex was reduced in the presence of endocytosis modulators and at low temperature, suggesting an energy-dependent mechanism consistent with endocytosis. On the whole, the biological activity evaluated herein suggests that the complex could be a promising anticancer agent.
authors: Centro de Ciências Moleculares e Materiais, Faculdade de Ciências da Universidade de Lisboa, Campo Grande, 1749-016 Lisboa, Portugal.
authors: Tânia S
authors: TS
authors: Morais
authors: Filipa
authors: F
authors: Santos
authors: Leonor
authors: L
authors: Côrte-Real
authors: Fernanda
authors: F
authors: Marques
authors: M Paula
authors: MP
authors: Robalo
authors: Paulo J Amorim
authors: PJ
authors: Madeira
authors: M Helena
authors: MH
authors: Garcia
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D056831:Coordination Complexes / Q000737:chemistry* / Q000494:pharmacology; D004563:Electrochemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D012428:Ruthenium / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D008024:Ligands; D012428:Ruthenium; D002945:Cisplatin