Journal
JOURNAL OF INORGANIC BIOCHEMISTRY
Volume 130, Issue -, Pages 32-37Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2013.09.019
Keywords
Antitumor properties; Gold(I); Aminophosphine ligands; Thiolate compounds; DNA binding; Thioredoxin reductase
Funding
- Ministerio de Economia y Competitividad [MEC/FEDER CTQ2010-20500-C02-01, BFU2012-31458]
- DGA-FSE [E77]
- [CSIC/FCT 20090048]
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Biological properties of a series of aminophosphine-thiolate gold(I) complexes [Au(SR)(PPh2NHPY)] [Ph2PNHPY = 2-(diphenylphosphinoamino)pyridine; HSR = 2-mercaptopyridine (2-HSpy) (3), 2-mercaptonicotinic acid (2-H-2-mna) (4), 2-thiouracil (2-HTU) (5) or 2-thiocytosine (2-HTC) (6)] and [Au(SR){PPh2NH(Htrz)}] [Ph2PNH(Htrz) = 3-(diphenylphosphinoamino)-1,2,4-triazole]; HSR = 2-mercaptopyridine (2-HSpy) (7), 2-thiocytosine (2-HTC) (8) or 6-thioguanine (6-HTG) (9) have been studied. Their antitumor properties have been tested in vitro against two tumor human cell lines, HeLa (derived from cervical cancer) and MCF-7 (derived from breast cancer), using a metabolic activity test (3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide, MTT). Some of them showed excellent cytotoxic activity. With the aim to obtain more information about the mechanisms of action of these derivatives, the interactions of complexes 3, 5, 7 and 9 with thioredoxin reductase in HeLa cells were studied. They showed a potent inhibition of thioredoxin reductase activity. In order to complete this study, interactions of the complexes with calf thymus (CT-) DNA and with different bacterial DNAs, namely the plasmid pEMBL9 and the promoter region of the furA (ferric uptake regulator A) gene from Anabaena sp. PCC 7120 were investigated. Although interactions of complexes with CT-DNA have been verified, none of them cause significant changes in its structure. (C) 2013 Elsevier Inc. All rights reserved.
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