Please use this identifier to cite or link to this item: https://scidar.kg.ac.rs/handle/123456789/8786
Title: In vitro antitumor activity, metal uptake and reactivity with ascorbic acid and BSA of some gold(III) complexes with N,N′-ethylenediamine bidentate ester ligands
Authors: Pantelić N.
Zmejkovski B.
Kolundžija B.
Djordjic Crnogorac, Marija
Vujic J.
Dojčinović, Biljana
Trifunović, Srećko
Stanojkovic, Tatjana
Sabo, Tibor
Kaluđerović, Goran
Issue Date: 2017
Abstract: © 2017 Elsevier Inc. Four novel gold(III) complexes of general formulae [AuCl2{(S,S)-R2eddl}]PF6 (R2eddl = O,O′-dialkyl-(S,S)-ethylenediamine-N,N′-di-2-(4-methyl)pentanoate, R = n-Pr, n-Bu, n-Pe, i-Bu; 1–4, respectively), were synthesized and characterized by elemental analysis, UV/Vis, IR, and NMR spectroscopy, as well as high resolution mass spectrometry. Density functional theory calculations pointed out that (R,R)-N,N′-configuration diastereoisomers were energetically the most favorable. Duo to high cytotoxic activity complex 3 was chosen for stability study in DMSO, no decomposition occurs within 24 h, and for the reaction with ascorbic acid in which was reduced immediately. Additionally, 3 interacts with bovine serum albumin (BSA) as proven by UV/Vis spectroscopy. In vitro antitumor activity was determined against human cervix adenocarcinoma (HeLa), human myelogenous leukemia (K562), and human melanoma (Fem-x) cancer cell lines, as well as against non-cancerous human embryonic lung fibroblast cells MRC-5. The highest activity was observed against K562 cells (IC50: 5.04–6.51 μM). Selectivity indices showed that these complexes are less toxic than cisplatin. 3 had a similar viability kinetics on HeLa cells as cisplatin. Drug accumulation studies in HeLa cells showed that the total gold uptake increased much faster than that of cisplatin pointing out that 3 more efficiently enters the cells than cisplatin. Furthermore, morphological and cell cycle analysis reveal that gold(III) complexes induced apoptosis in time- and dose-dependent manner.
URI: https://scidar.kg.ac.rs/handle/123456789/8786
Type: article
DOI: 10.1016/j.jinorgbio.2017.04.001
ISSN: 0162-0134
SCOPUS: 2-s2.0-85017584556
Appears in Collections:Faculty of Science, Kragujevac

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