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dc.contributor.author |
Melounková, Lucie
|
cze |
dc.contributor.author |
Machálková, Aneta
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cze |
dc.contributor.author |
Havelek, Radim
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cze |
dc.contributor.author |
Honzíček, Jan
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cze |
dc.contributor.author |
Rezacova, Martina
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cze |
dc.contributor.author |
Císařova, Ivana
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cze |
dc.contributor.author |
Peterova, Eva
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cze |
dc.contributor.author |
Vinklárek, Jaromír
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cze |
dc.date.accessioned |
2020-03-19T12:56:11Z |
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dc.date.available |
2020-03-19T12:56:11Z |
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dc.date.issued |
2019 |
eng |
dc.identifier.issn |
0162-0134 |
eng |
dc.identifier.uri |
https://hdl.handle.net/10195/74953 |
|
dc.description.abstract |
Ten new vanadocene complexes bearing N,N'-chelating ligands were prepared, characterized, and their cytotoxicity toward a panel of cancer cells was measured. Structures of four vanadocene compounds were determined by single crystal X-ray diffraction analysis. Complexes containing 1,2-bis(phenylimino)acenaphthene (bian) and 1,2-bis(4-methoxyphenylimino)acenaphthene (4-MeO-bian) exhibit higher cytotoxicity than those with dipyrido[3,2-a:2',3'-c]phenazine (dppz) and (E)-N-((pyridin-2-yl)methylene)benzenamine (pyma). In light of the finding, cytotoxic mechanisms of two highly effective complexes [(eta(5)-C5H4Me)(2)V(bian)][OTf](2) (3b) and [(eta(5)-C5H4Me)(2)V(4-MeO-bian)][OTf](2) (4b) against human A549 lung adenocarcinoma cells were investigated by following membrane leakage of intracellular lactate dehydrogenase, Trypan Blue staining and activation of tumor protein p53 (p53). Evaluated complexes have a potent dose-dependent antiproliferative activity, causing cell cycle redistribution by the increased accumulation of cells in the G2 and S phase. In accord with the observed cell cycle deceleration, cyclin-dependent kinase inhibitor-interacting protein 1 (p21(WAF1/Cip1)), extra cellular signal regulated kinases 1 and 2 (ERK1/2), Checkpoint kinase 1 (Chk1), Checkpoint kinase 2 (Chk2) and their phosphorylated forms Chk1 at serine 345 and Chk2 at threonine 68 increased. In the cells exposed to complexes, dose- and time-dependent apoptotic process is initiated by the activation of the initiator caspase 8, followed by activation of effector caspase 3/7 and phosphatidylserine externalization. Moreover, because of treatment, A549 cells activate prosurvival mitogen-activated protein kinases (MAPK) signaling and up-regulate antiapoptotic protein B-cell lymphoma (Bcl-2), thereby promoting evasion of cell death. Both complexes exhibited considerably higher cytotoxic effect than the reference anticancer drug cis-platin and the cytotoxicity was more pronounced at higher treatment time. |
eng |
dc.format |
p. 182-193 |
eng |
dc.language.iso |
eng |
eng |
dc.publisher |
Elsevier Science BV |
eng |
dc.relation.ispartof |
Journal of Inorganic Biochemistry, volume 195, issue: June |
eng |
dc.rights |
Text článku ve verzi postprint bude přístupný od 22.03.2021. |
eng |
dc.subject |
Vanadium(IV) |
eng |
dc.subject |
Cytotoxicity |
eng |
dc.subject |
Apoptosis |
eng |
dc.subject |
A549 lung adenocarcinoma cells |
eng |
dc.subject |
vanad |
cze |
dc.subject |
cytotoxicita |
cze |
dc.subject |
apoptóza |
cze |
dc.title |
Vanadocene complexes bearing N,N'-chelating ligands: Synthesis, structures and in vitro cytotoxic studies on the A549 lung adenocarcinoma cell line |
eng |
dc.title.alternative |
Vanadocenové komplexy s N,N-chelátujícími ligandy: Příprava, struktura a in vitro aktivita na buněčné linii A549 |
cze |
dc.type |
article |
eng |
dc.description.abstract-translated |
Nové vanadocenové komplexy s N,N-chelatujícími ligandy byly připraveny a charakterizovány. byla měřena jejich cytotoxicita vůči panelu nádorových buněk. Struktura 4 sloučenin byla stanovena RTG analýzou. Mechanismus cytotoxického účinku byl studován na dvou derivátech. |
cze |
dc.peerreviewed |
yes |
eng |
dc.publicationstatus |
postprint |
eng |
dc.identifier.doi |
10.1016/j.jinorgbio.2019.03.015 |
eng |
dc.relation.publisherversion |
https://www.sciencedirect.com/science/article/pii/S0162013418304574 |
eng |
dc.identifier.wos |
000469408500019 |
eng |
dc.identifier.obd |
39883239 |
eng |
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