| Name: | Description: | Size: | Format: | |
|---|---|---|---|---|
| 199.68 KB | Adobe PDF |
Advisor(s)
Abstract(s)
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.
Description
Keywords
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
Citation
MORAIS, Tania S.; SANTOS, Filipa; CORTE-REAL, Leonor; MARQUES, Fernanda; ROBALO, M. Paula; MADEIRA, Paulo J. Amorim; GARCIA, M. Helena - Biological activity and cellular uptake of [Ru(eta(5)-C5H5)(PPh3)(Me(2)bpy)][CF3SO3] complex. Journal of Inorganic Biochemistry. ISSN 0162-0134. Vol. 122(2013), p. 8-17.