| Texto completo | |
| Autor(es): |
Brooks, Lirka
;
Palmeira-Mello, Marcos, V
;
Fernandez, Carlos Y.
;
Arandia, Ines
;
Ellena, Javier
;
Costa-Filho, Antonio J.
;
Batista, Alzir A.
;
Alvarez, Natalia
;
Facchin, Gianella
Número total de Autores: 9
|
| Tipo de documento: | Artigo Científico |
| Fonte: | Journal of Inorganic Biochemistry; v. 274, p. 10-pg., 2026-01-01. |
| Resumo | |
The high incidence and mortality associated with cancer evidence the need for novel therapeutic agents. Metalbased coordination compounds offer a diverse arsenal of molecules that can be developed into drugs, beyond those currently in clinical use. Among them, copper complexes are emerging as promising candidates for cancer treatment. In this study, a series of complexes [Cu(L-dipeptide)(met-phen)] (where met-phen: 4-methyl-1,10phenanthroline and 5-methyl-1,10-phenanthroline) were synthesized and characterized. Solid-state characterization included the determination of the crystal structures of [Cu(Gly-Gly)(4met-phen)]center dot 5.5 H2O and [Cu(pheala)(4met-phen)]center dot 3H2O. DNA binding was assessed through the intrinsic binding constant (Kb) and relative viscosity measurements, indicating partial intercalation into calf-thymus DNA. The obtained Kb values were approximately tenfold lower than those reported for analogous complexes with phenanthroline. The cytotoxicity of the complexes was evaluated against a panel of human cancer cell lines: metastatic breast adenocarcinoma MDA-MB-231 (triple negative, ATCC: HTB-26), lung epithelial carcinoma A549 (ATCC: CCL-185), ovarian carcinoma A2780 (ECACC 93112519), and nontumoral lung cell line MRC-5 (ATCC: CCL-171). The complexes exhibited potent cytotoxicity, with IC50 values in the low micromolar range, which was significantly more effective than that of cisplatin. [Cu(ala-gly)(5met-phen)] inhibits clonogenic colony formation and induces cellular death above its IC50. These findings evidence that [Cu(L-dipeptide)(met-phen)] complexes are interesting candidates for further in vivo investigation. (AU) | |
| Processo FAPESP: | 23/02475-8 - Complexos fosfínicos de Ru(II) com naftoquinonas e derivados: potenciais anticancerígenos, estudos in vitro e in vivo |
| Beneficiário: | Alzir Azevedo Batista |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |
| Processo FAPESP: | 21/01787-0 - Estudo in vitro e in vivo de complexos fosfínicos de Ru(II) com atividades anticancerígenas |
| Beneficiário: | Marcos Vinícius Palmeira de Mello |
| Modalidade de apoio: | Bolsas no Brasil - Pós-Doutorado |
| Processo FAPESP: | 17/15850-0 - Difração de raios X como ferramenta no desenvolvimento de potenciais fármacos |
| Beneficiário: | Eduardo Ernesto Castellano |
| Modalidade de apoio: | Auxílio à Pesquisa - Temático |
| Processo FAPESP: | 22/02876-0 - Avaliação do perfil biológico de complexos de coordenação: uma abordagem em modelos celulares 2D e 3D |
| Beneficiário: | Fillipe Vieira Rocha |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |