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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
dc.creator | Pantelić, Nebojša | |
dc.creator | Zmejkovski, Bojana B. | |
dc.creator | Kolundzija, Branka | |
dc.creator | Dordić-Crnogorac, Marija | |
dc.creator | Vujić, Jelena M. | |
dc.creator | Dojčinović, Biljana | |
dc.creator | Trifunović, Srecko R. | |
dc.creator | Stanojković, Tatjana P. | |
dc.creator | Sabo, Tibor J. | |
dc.creator | Kaludjerović, Goran N. | |
dc.date.accessioned | 2020-12-17T21:53:40Z | |
dc.date.available | 2020-12-17T21:53:40Z | |
dc.date.issued | 2017 | |
dc.identifier.issn | 0162-0134 | |
dc.identifier.uri | http://aspace.agrif.bg.ac.rs/handle/123456789/4340 | |
dc.description.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 cells 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. | en |
dc.publisher | Elsevier Science Inc, New York | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172035/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/172016/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/Basic Research (BR or ON)/175011/RS// | |
dc.rights | restrictedAccess | |
dc.source | Journal of Inorganic Biochemistry | |
dc.subject | Gold(III) complexes | en |
dc.subject | R(2)edda-type ligands | en |
dc.subject | Metal uptake | en |
dc.subject | Apoptosis | en |
dc.subject | Biological reactivity | en |
dc.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 | en |
dc.type | article | |
dc.rights.license | ARR | |
dc.citation.epage | 66 | |
dc.citation.other | 172: 55-66 | |
dc.citation.rank | M22 | |
dc.citation.spage | 55 | |
dc.citation.volume | 172 | |
dc.identifier.doi | 10.1016/j.jinorgbio.2017.04.001 | |
dc.identifier.scopus | 2-s2.0-85017584556 | |
dc.identifier.pmid | 28433833 | |
dc.identifier.wos | 000404000300007 | |
dc.type.version | publishedVersion |