Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F23%3A73620094" target="_blank" >RIV/61989592:15640/23:73620094 - isvavai.cz</a>
Nalezeny alternativní kódy
RIV/61989592:15310/23:73620094
Výsledek na webu
<a href="https://www.mdpi.com/1999-4923/15/2/307" target="_blank" >https://www.mdpi.com/1999-4923/15/2/307</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/pharmaceutics15020307" target="_blank" >10.3390/pharmaceutics15020307</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity
Popis výsledku v původním jazyce
A series of six heteroleptic copper(II) complexes with 2 '-hydroxy-4-(dimethylamino)chalcone (HL) with the composition [Cu(N-N)(L)]NO3 (1-6), where N-N stands for dmbpy = 5,5 '-dimethyl-2,2 '-bipyridine (1), bphen = 4,7-diphenyl-1,10-phenanthroline (2), dbbpy = 4,4 '-di-tert-butyl-2,2 '-bipyridine (3), nphen = 5-nitro-1,10-phenanthroline (4), bpy = 2,2 '-bipyridine, (5), and dpa = 2,2 '-dipyridylamine (6), was prepared and thoroughly characterized. The in vitro cytotoxicity screening on eight human cancer cell lines identified complex 2, containing the bulkiest N-donor ligands (bphen) as highly cytotoxic against cancer cells, with IC50 values ranking from 1.0 to 2.3 mu M, with good selectivity and low toxicity against healthy human fetal lung fibroblasts MRC-5. The cell-based assays, involving the most effective complex 2 in A2780 cancer cells, revealed its strong pro-apoptotic effects based on the effective activation of caspases 3/7, ROS overproduction, and autophagy in the A2780 cells while not impeding the cell cycle and mitochondrial membrane functions. The cellular uptake studies in A2780 and 22Rv1 cells uncovered no intracellular transport of the cationic complex 2, supporting the hypothesis that the in vitro anticancer effects of complex 2 are based on the combined extrinsic activation of apoptosis and autophagy induction.
Název v anglickém jazyce
Heteroleptic Copper(II) Complexes Containing 2′-Hydroxy-4-(Dimethylamino)Chalcone Show Strong Antiproliferative Activity
Popis výsledku anglicky
A series of six heteroleptic copper(II) complexes with 2 '-hydroxy-4-(dimethylamino)chalcone (HL) with the composition [Cu(N-N)(L)]NO3 (1-6), where N-N stands for dmbpy = 5,5 '-dimethyl-2,2 '-bipyridine (1), bphen = 4,7-diphenyl-1,10-phenanthroline (2), dbbpy = 4,4 '-di-tert-butyl-2,2 '-bipyridine (3), nphen = 5-nitro-1,10-phenanthroline (4), bpy = 2,2 '-bipyridine, (5), and dpa = 2,2 '-dipyridylamine (6), was prepared and thoroughly characterized. The in vitro cytotoxicity screening on eight human cancer cell lines identified complex 2, containing the bulkiest N-donor ligands (bphen) as highly cytotoxic against cancer cells, with IC50 values ranking from 1.0 to 2.3 mu M, with good selectivity and low toxicity against healthy human fetal lung fibroblasts MRC-5. The cell-based assays, involving the most effective complex 2 in A2780 cancer cells, revealed its strong pro-apoptotic effects based on the effective activation of caspases 3/7, ROS overproduction, and autophagy in the A2780 cells while not impeding the cell cycle and mitochondrial membrane functions. The cellular uptake studies in A2780 and 22Rv1 cells uncovered no intracellular transport of the cationic complex 2, supporting the hypothesis that the in vitro anticancer effects of complex 2 are based on the combined extrinsic activation of apoptosis and autophagy induction.
Klasifikace
Druh
J<sub>imp</sub> - Článek v periodiku v databázi Web of Science
CEP obor
—
OECD FORD obor
21002 - Nano-processes (applications on nano-scale); (biomaterials to be 2.9)
Návaznosti výsledku
Projekt
Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.
Návaznosti
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Ostatní
Rok uplatnění
2023
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Pharmaceutics
ISSN
1999-4923
e-ISSN
—
Svazek periodika
15
Číslo periodika v rámci svazku
2
Stát vydavatele periodika
CH - Švýcarská konfederace
Počet stran výsledku
21
Strana od-do
—
Kód UT WoS článku
000940911000001
EID výsledku v databázi Scopus
2-s2.0-85149115450