Several novel copper (II) complexes of reduced Schiff bases containing fluoride substituents were prepared and structurally characterized by single-crystal X-ray diffraction. The complexes exhibited diverse structures, with the central atom in distorted tetrahedral geometry. The biological effects of the products were evaluated, specifically their cytotoxicity, antimicrobial, and antiurease activities, as well as affinity for albumin (BSA) and DNA (ct-DNA). The complexes showed marked cytotoxic activities in the HepG2 hepatocellular carcinoma cell line, considerably higher than the standard cisplatin. The cytotoxicity depended significantly on the substitution pattern. The best activity was observed in the complex with a trifluoromethyl group in position 4 of the benzene ring-the dichloro[(±)-trans-N,N'-bis-(4-trifluoromethylbenzyl)-cyclohexane-1,2-diamine]copper (II) complex, whose activity (IC50 28.7 μM) was higher than that of the free ligand and markedly better than the activity of the standard cisplatin (IC50 336.8 μM). The same complex also showed the highest antimicrobial effect in vitro. The affinity of the complexes towards bovine serum albumin (BSA) and calf thymus DNA (ct-DNA) was established as well, indicating only marginal differences between the complexes. In addition, all complexes were shown to be excellent inhibitors of the enzyme urease, with the IC50 values in the lower micromolar region.
- MeSH
- buňky Hep G2 MeSH
- DNA metabolismus chemie MeSH
- fluor chemie MeSH
- komplexní sloučeniny * farmakologie chemie chemická syntéza MeSH
- lidé MeSH
- ligandy MeSH
- měď * chemie MeSH
- protinádorové látky * farmakologie chemie MeSH
- Schiffovy báze * chemie farmakologie MeSH
- sérový albumin hovězí chemie MeSH
- ureasa antagonisté a inhibitory metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Predložená práca sa zaoberá izoláciou a identifikáciou obsahových látok prítomných v listoch drieňa lekárskeho (Cornus officinalis Sieb. et Zucc.). Z petroléterového extraktu listov tejto rastliny bol izolovaný β-sitosterol, z metanolového extraktu glukóza a sacharóza a z vodno-metanolového extraktu kyselina galová, kvercetín a kvercetín-3-O-glukozid (izokvercitrín). Izolované látky boli identifikované pomocou fyzikálno-chemických metód, porovnaním výsledkov so štandardami a literatúrou. Z listov Cornus officinalis Sieb. et Zucc. boli látky I–V izolované prvýkrát.
The paper deals with the isolation and identification of the constituents of Cornus officinalis Sieb. et Zucc. leaves. There was isolated β-sitosterol from petroleum ether extract, glucose and saccharose from methanolic extract and gallic acid, quercetin and quercetin-3-O-glucoside (isoquercitrin) from aqueous-methanolic extract. Isolates were identified by physico-chemical data, and by comparing with authentic samples and literature data. The compounds I – V were isolated from the leaves of Cornus officinalis Sieb. et Zucc. for the first time.
