Copper (II) Species with Improved Anti-Melanoma and Antibacterial Activity by Inclusion in β-Cyclodextrin
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Chemistry
Molecular Biology
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To improve their biological activity, complexes [Cu(bipy)(dmtp)(OH)](ClO)·dmtp () and [Cu(phen)(dmtp)(OH)](ClO)·dmtp () (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 (O· 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 ()@β-CD in comparison with (). This behavior is associated with a cell cycle arrest in the G0/G1 phase. Compared with precursors, ()@β-CD and ()@β-CD exhibit 17 and 26 times more intense activity against planktonic , respectively, while ()@β-CD is 3 times more active against the strain.
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