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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F14%3A33152238%21RIV15-MSM-15310___
rdf:type
n6:Vysledek skos:Concept
rdfs:seeAlso
http://www.plosone.org/article/fetchObject.action?uri=info:doi/10.1371/journal.pone.0107373&representation=PDF
dcterms:description
A series of gold(I) complexes involving triphenylphosphine (PPh3) and one N-donor ligand derived from deprotonated mono-or disubstituted hypoxanthine (HLn) of the general composition [Au(Ln)(PPh3)] (1-9) is reported. The complexes were thoroughly characterized, including multinuclear high resolution NMR spectroscopy as well as single crystal X-ray analysis (for complexes 1 and 3). The complexes were screened for their in vitro cytotoxicity against human cancer cell lines MCF7 (breast carcinoma), HOS (osteosarcoma) and THP-1 (monocytic leukaemia), which identified the complexes 4-6 as the most promising representatives, who antiproliferative activity was further tested against A549 (lung adenocarcinoma), G-361 (melanoma), HeLa (cervical cancer), A2780 (ovarian carcinoma), A2780R (ovarian carcinoma resistant to cisplatin), 22Rv1 (prostate cancer) cell lines. Complexes 4-6 showed a significantly higher in vitro anticancer effect against the employed cancer cells, except for G-361, as compared with the commercially used anticancer drug cisplatin, with IC50 approximate to 1-30 mu M. Antiinflammatory activity was evaluated in vitro by the assessment of the ability of the complexes to modulate secretion of the pro-inflammatory cytokines, i.e. tumour necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta), in the lipopolysaccharide-activated macrophage-like THP-1 cell model. The results of this study identified the complexes as auspicious antiinflammatory agents with similar or better activity as compared with the clinically applied gold-based antiarthritic drug Auranofin. In an effort to explore the possible mechanisms responsible for the biological effect, the products of interactions of selected complexes with sulfur-containing biomolecules (L-cysteine and reduced glutathione) were studied by means of the mass-spectrometry study. A series of gold(I) complexes involving triphenylphosphine (PPh3) and one N-donor ligand derived from deprotonated mono-or disubstituted hypoxanthine (HLn) of the general composition [Au(Ln)(PPh3)] (1-9) is reported. The complexes were thoroughly characterized, including multinuclear high resolution NMR spectroscopy as well as single crystal X-ray analysis (for complexes 1 and 3). The complexes were screened for their in vitro cytotoxicity against human cancer cell lines MCF7 (breast carcinoma), HOS (osteosarcoma) and THP-1 (monocytic leukaemia), which identified the complexes 4-6 as the most promising representatives, who antiproliferative activity was further tested against A549 (lung adenocarcinoma), G-361 (melanoma), HeLa (cervical cancer), A2780 (ovarian carcinoma), A2780R (ovarian carcinoma resistant to cisplatin), 22Rv1 (prostate cancer) cell lines. Complexes 4-6 showed a significantly higher in vitro anticancer effect against the employed cancer cells, except for G-361, as compared with the commercially used anticancer drug cisplatin, with IC50 approximate to 1-30 mu M. Antiinflammatory activity was evaluated in vitro by the assessment of the ability of the complexes to modulate secretion of the pro-inflammatory cytokines, i.e. tumour necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1 beta), in the lipopolysaccharide-activated macrophage-like THP-1 cell model. The results of this study identified the complexes as auspicious antiinflammatory agents with similar or better activity as compared with the clinically applied gold-based antiarthritic drug Auranofin. In an effort to explore the possible mechanisms responsible for the biological effect, the products of interactions of selected complexes with sulfur-containing biomolecules (L-cysteine and reduced glutathione) were studied by means of the mass-spectrometry study.
dcterms:title
Gold(I)-Triphenylphosphine Complexes with Hypoxanthine-Derived Ligands: In Vitro Evaluations of Anticancer and Anti-Inflammatory Activities Gold(I)-Triphenylphosphine Complexes with Hypoxanthine-Derived Ligands: In Vitro Evaluations of Anticancer and Anti-Inflammatory Activities
skos:prefLabel
Gold(I)-Triphenylphosphine Complexes with Hypoxanthine-Derived Ligands: In Vitro Evaluations of Anticancer and Anti-Inflammatory Activities Gold(I)-Triphenylphosphine Complexes with Hypoxanthine-Derived Ligands: In Vitro Evaluations of Anticancer and Anti-Inflammatory Activities
skos:notation
RIV/61989592:15310/14:33152238!RIV15-MSM-15310___
n3:aktivita
n16:S n16:P
n3:aktivity
P(ED2.1.00/03.0058), P(LO1305), S
n3:cisloPeriodika
9
n3:dodaniDat
n7:2015
n3:domaciTvurceVysledku
n4:4192478 n4:4373510 n4:2321459 n4:5059550 n4:8069239 n4:9388540
n3:druhVysledku
n11:J
n3:duvernostUdaju
n10:S
n3:entitaPredkladatele
n20:predkladatel
n3:idSjednocenehoVysledku
18474
n3:idVysledku
RIV/61989592:15310/14:33152238
n3:jazykVysledku
n18:eng
n3:klicovaSlova
cytotoxicity; auranofin; gold; X-ray structures; guanine derivatives; biological-activity
n3:klicoveSlovo
n5:biological-activity n5:gold n5:cytotoxicity n5:guanine%20derivatives n5:X-ray%20structures n5:auranofin
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[0381EA47AAF7]
n3:nazevZdroje
PLoS One
n3:obor
n13:CA
n3:pocetDomacichTvurcuVysledku
6
n3:pocetTvurcuVysledku
6
n3:projekt
n17:ED2.1.00%2F03.0058 n17:LO1305
n3:rokUplatneniVysledku
n7:2014
n3:svazekPeriodika
9
n3:tvurceVysledku
Trávníček, Zdeněk Křikavová, Radka Hutyra, Jakub Hošek, Jan Dvořák, Zdeněk Vančo, Ján
n3:wos
000344317700050
s:issn
1932-6203
s:numberOfPages
13
n14:doi
10.1371/journal.pone.0107373
n15:organizacniJednotka
15310