Anticancer and Antibacterial Activity Studies of Gold(I)-Alkynyl Chromones
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Data
2015Autor
Szczupak, Łukasz
Hikisz, Paweł
Koceva-Chyla, Aneta
Kowalski, Konrad
Guśpiel, Adam
Solecka, Jolanta
Therrien, Bruno
Ott, Ingo
Oehninger, Luciano
Metadata
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Three gold(I) complexes of alkynyl chromones were synthesized and characterized. The
single-crystal X-ray structure analysis of a dinuclear compound and of a flavone derivative exhibit
a typical d10 gold(I)-alkynyl linear arrangement. All complexes were evaluated as anticancer and
antibacterial agents against four human cancer cell lines and four pathogenic bacterial strains. All
compounds show antiproliferative activity at lower micromolar range concentrations. Complex 4
showed a broad activity profile, being more active than the reference drug auranofin against HepG2,
MCF-7 and CCRF-CEM cancer cells. The cellular uptake into MCF-7 cells of the investigated
complexes was measured by atomic absorption spectroscopy (AAS). These measurements showed
a positive correlation between an increased cellular gold content and the incubation time of
the complexes. Unexpectedly an opposite effect was observed for the most active compound.
Biological assays revealed various molecular mechanisms for these compounds, comprising: (i)
thioredoxin reductase (TrxR) inhibition, (ii) caspases-9 and -3 activation; (iii) DNA damaging
activity and (iv) cell cycle disturbance. The gold(I) complexes were also bactericidal against
Gram-positive methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant S. aureus
(MRSA) bacterial strains, while showing no activity against the Gram-negative Escherichia coli
bacterial strain.
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