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  • A series of considerably anti-inflammatory active gold(I) mixed-ligand complexes, involving the benzylsubstituted derivatives of N6-benzyladenine (HLn) and triphenylphosphine (PPh3) as ligands and having the general formula [Au(Ln)(PPh3)]xH2O (1-4; n = 1-4 and x = 0-1), was evaluated for the ability to influence the expression of CYP1A1/2 and CYP3A4 and transcriptional activity of glucocorticoid (GR) and aryl hydrocarbon (AhR) receptors in primary human hepatocytes and HepG2 cells. In both tests, evaluating the ability of the complexes to modulate the expression of CYP1A1, CYP1A2 and CYP3A4 in primary human hepatocytes and influence the transcriptional activity of AhR and GR in the reporter cell lines, no negative influence on the major drug-metabolizing cytochrome P450 isoenzymes and their signaling pathway (through GR and AhR receptors) was observed. These positive findings revealed another substantial evidence that could lead to utilization of the complexes as effective and relatively safe drugs for the treatment of hard-to-treat inflammation-related diseases, such as rheumatoid arthritis, comparable or even better than clinically used gold-containing drug Auranofin.
  • A series of considerably anti-inflammatory active gold(I) mixed-ligand complexes, involving the benzylsubstituted derivatives of N6-benzyladenine (HLn) and triphenylphosphine (PPh3) as ligands and having the general formula [Au(Ln)(PPh3)]xH2O (1-4; n = 1-4 and x = 0-1), was evaluated for the ability to influence the expression of CYP1A1/2 and CYP3A4 and transcriptional activity of glucocorticoid (GR) and aryl hydrocarbon (AhR) receptors in primary human hepatocytes and HepG2 cells. In both tests, evaluating the ability of the complexes to modulate the expression of CYP1A1, CYP1A2 and CYP3A4 in primary human hepatocytes and influence the transcriptional activity of AhR and GR in the reporter cell lines, no negative influence on the major drug-metabolizing cytochrome P450 isoenzymes and their signaling pathway (through GR and AhR receptors) was observed. These positive findings revealed another substantial evidence that could lead to utilization of the complexes as effective and relatively safe drugs for the treatment of hard-to-treat inflammation-related diseases, such as rheumatoid arthritis, comparable or even better than clinically used gold-containing drug Auranofin. (en)
Title
  • Influence of gold(I) complexes involving adenine derivatives on major drug-drug interaction pathway
  • Influence of gold(I) complexes involving adenine derivatives on major drug-drug interaction pathway (en)
skos:prefLabel
  • Influence of gold(I) complexes involving adenine derivatives on major drug-drug interaction pathway
  • Influence of gold(I) complexes involving adenine derivatives on major drug-drug interaction pathway (en)
skos:notation
  • RIV/61989592:15310/13:33147829!RIV14-GA0-15310___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(ED2.1.00/03.0058), P(EE2.3.20.0017), P(GBP303/12/G163), S
http://linked.open...iv/cisloPeriodika
  • 8
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 79778
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15310/13:33147829
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Gold complexes, Cytochrome P450, Aryl hydrocarbon receptor, Glucocorticoid receptor, Drug-drug interactions (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [7A8C0F969C58]
http://linked.open...i/riv/nazevZdroje
  • Toxicology in Vitro
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 27
http://linked.open...iv/tvurceVysledku
  • Dvořák, Zdeněk
  • Novotná, Aneta
  • Trávníček, Zdeněk
  • Vančo, Ján
http://linked.open...ain/vavai/riv/wos
  • 000328723100028
issn
  • 0887-2333
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.tiv.2013.10.008
http://localhost/t...ganizacniJednotka
  • 15310
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