1. Copper (II) Species with Improved Anti-Melanoma and Antibacterial Activity by Inclusion in β-Cyclodextrin.
- Author
-
Tirsoaga A, Cojocaru V, Badea M, Badea IA, Rostas AM, Stoica R, Bacalum M, Chifiriuc MC, and Olar R
- Subjects
- Animals, Mice, Crystallography, X-Ray, Anti-Bacterial Agents pharmacology, Spectrophotometry, Infrared, Copper chemistry, beta-Cyclodextrins pharmacology, beta-Cyclodextrins chemistry
- Abstract
To improve their biological activity, complexes [Cu(bipy)(dmtp)
2 (OH2 )](ClO4 )2 ·dmtp ( 1 ) and [Cu(phen)(dmtp)2 (OH2 )](ClO4 )2 ·dmtp ( 2 ) (bipy 2,2'-bipyridine, phen: 1,10-phenantroline, and dmtp: 5,7-dimethyl-1,2,4-triazolo [1,5-a]pyrimidine) were included in β-cyclodextrins (β-CD). During the inclusion, the co-crystalized dmtp molecule was lost, and UV-Vis spectra together with the docking studies indicated the synthesis of new materials with 1:1 and 1:2 molar ratios between complexes and β-CD. The association between Cu(II) compounds and β-CD has been proven by the identification of the components' patterns in the IR spectra and powder XRD diffractograms, while solid-state UV-Vis and EPR spectra analysis highlighted a slight modification of the square-pyramidal stereochemistry around Cu(II) in comparison with precursors. The inclusion species are stable in solution and exhibit the ability to scavenge or trap ROS species (O2 ·- and HO·) as indicated by the EPR experiments. Moreover, the two inclusion species exhibit anti-proliferative activity against murine melanoma B16 cells, which has been more significant for ( 2 )@β-CD in comparison with ( 2 ). This behavior is associated with a cell cycle arrest in the G0/G1 phase. Compared with precursors, ( 1a )@β-CD and ( 2a )@β-CD exhibit 17 and 26 times more intense activity against planktonic Escherichia coli , respectively, while ( 2a )@β-CD is 3 times more active against the Staphylococcus aureus strain.- Published
- 2023
- Full Text
- View/download PDF