Exploring the therapeutic potential of Cu(II)-complexes with ligands derived from pyridoxal

Nunes, Patrique; Marques, Fernanda; Cavaco, Isabel; Pessoa, Joao Costa; Correia, Isabel

http://hdl.handle.net/10400.1/16449

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Abstract(s)

Three new copper(II) complexes formulated as [Cu(L)(X)], where X = H2O or Cl and H2L is a Schiff base (H2L1,2) or its reduced version ((H3LCl)-Cl-3) derived from pyridoxal, are prepared, as well as two ternary complexes [Cu(L) (phen)] also containing 1,10-phenanthroline. All compounds are characterized by the usual techniques: elemental analyses, ESI mass spectrometry, UV-Vis absorption, FTIR and EPR spectroscopies. The ligands co-ordinate the Cu(II) center forming complexes with square-planar based geometries. Their antioxidant properties are evaluated with a radical scavenging activity assay, with one of the ligand precursors showing activity higher than the positive control, ascorbic acid. The antiproliferative activity of all compounds is evaluated against two cancer cell lines: ovarian (A2780) and breast (MCF7). All complexes show moderate to excellent activity with the ternary Cu-complexes showing IC50 values between 0.7 and 9.3 mu M after 24 h of incubation, values much lower than those reported for cisplatin, the reference drug. The hydrolytic stability of the complexes and their ability to bind albumin and DNA are evaluated by spectroscopic techniques, showing that the compounds bind bovine serum albumin. The [Cu(L)(phen)] complexes show ability to target DNA via intercalation.