Copper (II) Species with Improved Anti-Melanoma and Antibacterial Activity by Inclusion in β-Cyclodextrin

To improve their biological activity, complexes [Cu(bipy)(dmtp)<sub>2</sub>(OH<sub>2</sub>)](ClO<sub>4</sub>)<sub>2</sub>·dmtp (<b>1</b>) and [Cu(phen)(dmtp)<sub>2</sub>(OH<sub>2</sub>)](ClO<sub>4</sub>)&...

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Bibliographic Details
Main Authors: Alina Tirsoaga, Victor Cojocaru, Mihaela Badea, Irinel Adriana Badea, Arpad Mihai Rostas, Roberta Stoica, Mihaela Bacalum, Mariana Carmen Chifiriuc, Rodica Olar
Format: Article
Language:English
Published: MDPI AG 2023-01-01
Series:International Journal of Molecular Sciences
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Online Access:https://www.mdpi.com/1422-0067/24/3/2688
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Summary:To improve their biological activity, complexes [Cu(bipy)(dmtp)<sub>2</sub>(OH<sub>2</sub>)](ClO<sub>4</sub>)<sub>2</sub>·dmtp (<b>1</b>) and [Cu(phen)(dmtp)<sub>2</sub>(OH<sub>2</sub>)](ClO<sub>4</sub>)<sub>2</sub>·dmtp (<b>2</b>) (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<sub>2</sub>·<sup>−</sup> 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 (<b>2</b>)@β-CD in comparison with (<b>2</b>). This behavior is associated with a cell cycle arrest in the G0/G1 phase. Compared with precursors, (<b>1a</b>)@β-CD and (<b>2a</b>)@β-CD exhibit 17 and 26 times more intense activity against planktonic <i>Escherichia coli</i>, respectively, while (<b>2a</b>)@β-CD is 3 times more active against the <i>Staphylococcus aureus</i> strain.
ISSN:1661-6596
1422-0067