Tuning the Biological Activity of Camphorimine Complexes through Metal Selection

Tuning the Biological Activity of Camphorimine Complexes through Metal Selection

The cytotoxic activity of four sets of camphorimine complexes based on the Cu(I), Cu(II), Ag(I), and Au(I) metal sites were assessed against the cisplatin-sensitive A2780 and OVCAR3 ovarian cancer cells. The results showed that the gold complexes were ca. one order of magnitude more active than the...

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Published in:Antibiotics (Basel) Vol. 11; no. 8; p. 1010
Main Authors: Costa, Joana P., Pinheiro, Teresa, Martins, Maria S., Carvalho, M. Fernanda N. N., Feliciano, Joana R., Leitão, Jorge H., Silva, Rafaela A. L., Guerreiro, Joana F., Alves, Luís M. C., Custódio, Inês, Cruz, João, Marques, Fernanda
Format: Journal Article
Language:English
Published: Basel MDPI AG 27-07-2022
MDPI
Subjects:
Biocompatibility
Biological activity
camphorimine complexes
Cancer therapies
Chemotherapy
Cisplatin
Copper
Copper compounds
cytotoxic activity
Cytotoxicity
Drugs
Emission
Fibroblasts
Gold
Ligands
Mitochondrial DNA
Nematodes
Ovarian cancer
PIXE
Reactive oxygen species
ROS
Selectivity
Signal transduction
Silver
Silver compounds
Toxicity
United Kingdom
Portugal
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Summary:The cytotoxic activity of four sets of camphorimine complexes based on the Cu(I), Cu(II), Ag(I), and Au(I) metal sites were assessed against the cisplatin-sensitive A2780 and OVCAR3 ovarian cancer cells. The results showed that the gold complexes were ca. one order of magnitude more active than the silver complexes, which in turn were ca. one order of magnitude more active than the copper complexes. An important finding was that the cytotoxic activity of the Ag(I) and Au(I) camphorimine complexes was higher than that of cisplatin. Another relevant aspect was that the camphorimine complexes did not interact significantly with DNA, in contrast with cisplatin. The cytotoxic activity of the camphorimine complexes displayed a direct relationship with the cellular uptake by OVCAR3 cells, as ascertained by PIXE (particle-induced X-ray emission). The levels of ROS (reactive oxygen species) formation exhibited an inverse relationship with the reduction potentials for the complexes with the same metal, as assessed by cyclic voltammetry. In order to gain insight into the toxicity of the complexes, their cytotoxicity toward nontumoral cells (HDF and V79 fibroblasts) was evaluated. The in vivo cytotoxicity of complex 5 using the nematode Caenorhabditis elegans was also assessed. The silver camphorimine complexes displayed the highest selectivity coefficients (activity vs. toxicity).
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ISSN:2079-6382
2079-6382
DOI:10.3390/antibiotics11081010