Gold(I) N-heterocyclic carbene complexes show strong proapoptotic, antioxidant and anti-inflammatory effects in A2780 and endothelial cells
Jazyk angličtina Země Irsko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
39824433
DOI
10.1016/j.cbi.2025.111381
PII: S0009-2797(25)00011-0
Knihovny.cz E-zdroje
- Klíčová slova
- A2780, Anti-inflammatory, Cellular effects, Cytotoxicity, Gold, NHC, Proteomics,
- MeSH
- antiflogistika * farmakologie chemie MeSH
- antioxidancia * farmakologie chemie MeSH
- apoptóza * účinky léků MeSH
- endoteliální buňky pupečníkové žíly (lidské) účinky léků MeSH
- endoteliální buňky účinky léků metabolismus cytologie MeSH
- heterocyklické sloučeniny * chemie MeSH
- komplexní sloučeniny * chemie farmakologie MeSH
- lidé MeSH
- methan * analogy a deriváty chemie farmakologie MeSH
- nádorové buněčné linie MeSH
- protinádorové látky farmakologie chemie MeSH
- zlato * chemie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antiflogistika * MeSH
- antioxidancia * MeSH
- carbene MeSH Prohlížeč
- heterocyklické sloučeniny * MeSH
- komplexní sloučeniny * MeSH
- methan * MeSH
- protinádorové látky MeSH
- zlato * MeSH
A series of eight gold(I) N-heterocyclic carbene (NHC) complexes [Au(IMes)(Ln)] based on 1,3-bis(2,4,6-trimethylphenyl)imidazole-2-ylidene (IMes) and 7-azaindole derivatives (HLn), where n = 1-8 for HL1 = 5-fluoro-7-azaindole, HL2 = 5-bromo-7-azaindole, HL3 = 3-chloro-7-azaindole, HL4 = 3-iodo-7-azaindole, HL5 = 5-bromo-3-chloro-7-azaindole, HL6 = 5-bromo-3-iodo-7-azaindole, HL7 = 4-chloro-2-methyl-7-azaindole and HL8 = 7-azaindole, was prepared, characterised and studied for their in vitro anti-cancer and anti-inflammatory effects. The complexes showed significant cytotoxicity on human ovarian cancer cell lines (A2780, IC50 ≈ 8-19 μM and A2780R, IC50 ≈ 8-19 μM) and lowered toxicity in normal HaCat and MRC-5 cells. Cellular effects of the selected complexes 1 and 7 were evaluated in A2780 cells using flow cytometry. Moreover, the time-dependent cellular uptake in A2780 cells, a shotgun proteomic analysis, an ESI-MS study of hydrolysis and interactions with l-cysteine and reduced glutathione (GSH) were performed. Complexes 1 and 7 revealed remarkable anti-inflammatory effects via inhibition of NF-κB activity in human endothelial cells.
Citace poskytuje Crossref.org
