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.

journal_name

J Inorg Biochem

authors

Morais TS,Santos F,Côrte-Real L,Marques F,Robalo MP,Madeira PJ,Garcia MH

doi

10.1016/j.jinorgbio.2013.01.011

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

8-17

eissn

0162-0134

issn

1873-3344

pii

S0162-0134(13)00026-3

journal_volume

122

pub_type

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