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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

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Authors
Pantelić, Nebojša Đ.
Zmejkovski, Bojana
Kolundžija, Branka
Crnogorac, Marija Đorđić
Vujić, Jelena M.
Dojčinović, Biljana
Trifunović, Srećko R.
Stanojković, Tatjana
Sabo, Tibor
Kaluđerović, Goran N.
Article (Accepted Version)
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Abstract
Four novel gold(III) complexes of general formulae [AuCl2{(S,S)-R(2)eddl}]PF6 (R(2)eddl = 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 cell...s MRC-5. The highest activity was observed against K562 cells (IC50: 5.04-6.51 mu M). 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.

Keywords:
Apoptosis / Biological reactivity / Gold(III) complexes / Metal uptake / R 2 edda-type ligands
Source:
Journal of Inorganic Biochemistry, 2017, 172, 55-66
Publisher:
  • Elsevier Science Inc, New York
Projects:
  • Rational design and synthesis of biologically active and coordination compounds and functional materials, relevant for (bio)nanotechnology (RS-172035)
  • Synthesis, modeling, physicochemical and biological properties of organic compounds and related metal complexes (RS-172016)
  • Biological response modifiers in physiological and pathological conditions (RS-175011)
Note:
  • This is the peer-reviewed version of the following article: Pantelić, N.; Zmejkovski, B. B.; Kolundžija, B.; Crnogorac, M. Đ.; Vujić, J. M.; Dojčinović, B.; Trifunović, S. R.; Stanojković, T. P.; Sabo, T. J.; Kaluđerović, G. N. 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. Journal of Inorganic Biochemistry 2017, 172, 55–66. https://doi.org/10.1016/j.jinorgbio.2017.04.001
  • http://cer.ihtm.bg.ac.rs/handle/123456789/2248

DOI: 10.1016/j.jinorgbio.2017.04.001

ISSN: 0162-0134

PubMed: 28433833

WoS: 000404000300007

Scopus: 2-s2.0-85017584556
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/2931
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