Biological activity and cellular uptake of [Ru(eta(5)-C5H5)(PPh3)(Me(2)bpy)][CF3SO3] complex

Anticancer activity of the new [Ru(eta(5)-C5H5)(PPh3)(Me(2)bpy)][CF3SO3] (Me(2)bpy = 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 nano...

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Bibliographic Details
Main Author: Morais, Tania S. (author)
Other Authors: Santos, Filipa (author), Côrte-Real, Leonor (author), Marques, Fernanda (author), Robalo, Maria Paula (author), Paulo J. Amorim Madeira (author), Garcia, M. Helena (author)
Format: article
Language:eng
Published: 2013
Subjects:
Ruthenium
Cyclopentadienyl
Cytotoxicity
Endocytosis modulators
Albumin
Fluorescence
Humam-Serum-Albumin
Cyclopentadienyl Derivative Complexes
In-Vitro
Heteroaromatic Ligands
Ruthenium Complexes
Arene Complexes
DNA Interaction
PTA Complexes
Binding-Sites
Cancer
Online Access:http://hdl.handle.net/10400.21/2865
Country:Portugal
Oai:oai:repositorio.ipl.pt:10400.21/2865
Description
Summary:Anticancer activity of the new [Ru(eta(5)-C5H5)(PPh3)(Me(2)bpy)][CF3SO3] (Me(2)bpy = 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(eta(5)-C5H5)(PPh3)(Me(2)bpy)][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. (C) 2013 Elsevier Inc. All rights reserved.

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