Author:
Machado Pedro Henrique Alves,Paixão Drielly Aparecida,Lino Ricardo Campos,de Souza Tiago Rodrigues,de Souza Bontempo Nayara Júnia,Sousa Luana Munique,Van Petten de Vasconcelos Azevedo Fernanda,Orsolin Priscila Capelari,Lima Paula Marynella Alves Pereira,Martins Isabella Castro,da Costa Guerra Joyce Ferreira,Teixeira Samuel Cota,Araújo Thaise Gonçalves,Goulart Luiz Ricardo,Morelli Sandra,Guerra Wendell,de Oliveira Júnior Robson José
Abstract
AbstractThe thin line between efficacy and toxicity has challenged cancer therapy. As copper is an essential micronutrient and is important to tumor biology, CuII complexes emerged as an alternative to chemotherapy; however, its biological properties need to be better understood. Thus, we report in vitro the antitumor effects of two CuII complexes named [Cu(4-fh)(phen)(ClO4)2] (complex 1) and [Cu(4-nh)(phen)(ClO4)2]·H2O (complex 2), in which 4-fh = 4-fluorophenoxyacetic acid hydrazide; 4-nh = 4-nitrobenzoic hydrazide and phen = 1,10-phenanthroline. Both complexes presented cytotoxic activity against tumor cells, but only complex 1 showed significant selectivity. Complex 1 also induced DNA-damage, led to G0/G1 arrest and triggered apoptosis, which was initiated by an autophagy dysfunction. The significant in vitro selectivity and the action mechanism of complex 1 are noteworthy and reveal this prodrug as promising for anticancer therapy.
Funder
Fundação de Amparo à Pesquisa do Estado de Minas Gerais
Conselho Nacional de Desenvolvimento Científico e Tecnológico
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - Brasil
Publisher
Springer Science and Business Media LLC
Cited by
10 articles.
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