Wydział Chemii

Valeria Ferretti

Cristina P. Matos

Catarina Canelas

João Costa Pessoa

Ana Isabel Tomaz

Radosław Starosta

Isabel Correia

Ignacio E. León

2022

Journal of Inorganic Biochemistry

236

111961/1-111961/14

10.1016/j.jinorgbio.2022.111961

Naukowa

Angielski

Artykuł

Due to the growing prevalence of cancer diseases, new therapeutic options are urgently needed, and drugs based on metal ions other than platinum are alternatives with exciting possibilities. We report the synthesis, characterization and biological effect of mixed-ligand Fe(III)-aminophenolate complexes derived from salicylaldehyde and L-tryptophan with quinoline derivatives as co-ligands, namely 8-hydroxyquinoline (8HQ), [Fe(L)(8HQ)(H₂O)] (1) and its 5-cloro derivative (Cl8HQ), [Fe(L)(Cl8HQ)(H₂O)] (2). The complex bearing the aminophenolate and lacking the quinoline co-ligand, [Fe(L)(Cl)(H₂O)₂] (3), was prepared for comparison. The analytical and spectroscopic characterization revealed that 1 and 2 are octahedral Fe(III) complexes with the aminophenolate acting as a dianionic tridentate ligand and 8HQ co-ligands as bidentate chelates. Spectroscopic techniques and molecular docking studies were used to evaluate the ability of these complexes to bind bovine serum albumin (BSA) and calf thymus DNA. Complex 2 [Fe(L)(Cl8HQ)(H₂O)] was the one showing higher affinity for both biomolecules. Cell viability was assessed in breast, colorectal and bone human cancer cell lines. 1 and 2 were found to be more active than cisplatin in all cell lines tested. A non-tumoral fibroblast line (L929, mouse non-tumoral fibroblasts) was used to evaluate selectivity. The results evidence that 2 shows much higher selectivity than 1 in all cell lines tested, but particularly in bone cancer cells in which selectivity index (SI) values are 8.0 and 18.8 for 1 and 2, respectively.

Aminophenolate, Reduced Schiff bases, Hydroxyquinolines, Fe-complexes, Selectivity, Anticancer activity

http://dx.doi.org/10.1016/j.jinorgbio.2022.111961

http://www.elsevier.com