4.7 Article

New Copper Complexes with Antibacterial and Cytotoxic Activity

Journal

Publisher

MDPI
DOI: 10.3390/ijms241813819

Keywords

Cu+2 complexes; crystal structure; antibacterial; cytotoxicity

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The discovery of new non-toxic metal complexes with biological activity is an active area of research. Two Cu+2 complexes with new ligands were synthesized and characterized by X-ray crystallography. Both complexes showed in vitro biological activities, with complex C2 being more active. The complexes exhibited distorted square pyramidal square-planar geometries and were characterized by FT-IR and UV-Vis spectroscopy. The antibacterial activity of the complexes against four Gram-positive and two Gram-negative bacteria was determined using the microdilution method, and cytotoxicity studies were carried out on tumor cell lines and a normal cell line. Flow cytometric assessment of apoptosis induced by the complexes was also performed.
The discovery of a new non-toxic metal complex with biological activity represents a very active area of research. Two Cu+2 complexes, [Cu-4(L1)(4)(OH)(4)(DMF)(2)(H2O)] (C1) (HL1 = N-(5-ethyl-[1,3,4]-thiadiazole-2-yl)-benzenesulfonamide) and [Cu(L2)(2)(phen)(H2O)] (C2) (HL2 = N-(5-(4-methylphenyl)-[1,3,4]-thiadiazole-2-yl)-naphtalenesulfonamide), with two new ligands were synthesized. The X-ray crystal structures of the complexes were determined. In both complexes, Cu+2 is five-coordinated, forming a CuN2O3 and CuN4O chromophore, respectively. The ligands act as monodentate, coordinating the metal ion through a single N-thiadiazole atom; for the two complexes, the molecules from the reaction medium (phenantroline, dimethylformamide and water) are also involved in the coordination of Cu+2. The complexes have a distorted square pyramidal square-planar geometry. The compounds were characterized by FT-IR and UV-Vis spectroscopy. Using the microdilution method, the antibacterial activity of the complexes was determined against four Gram-positive and two Gram-negative bacteria, with Gentamicin as the positive control. Cytotoxicity studies were carried out on two tumor cell lines (HeLa, DLD-1) and on a normal cell line (HFL1) using the MTT method and Cisplatin as a positive control. Flow cytometric assessment of apoptosis induced by the complexes on the three cell lines was also performed. Both complexes present in vitro biological activities but complex C2 is more active.

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