| Texto completo | |
| Autor(es): Mostrar menos - |
Ahmad, Atif
;
Graminha, Angelica Ellen
;
Anam
;
Nazir, Afaq
;
Abe, Saulo H. Mendes
;
Palmeira-Mello, Marcos V.
;
Dutra, Jocely L.
;
Badaro, Wladimir P. D.
;
Lazzarini, Ana Beatriz
;
de Moura, Thales Reggiani
;
Khan, Sabir
;
Batista, Alzir Azevedo
;
Netto, Adelino V. G.
;
Pereira, Jose Clayston Melo
Número total de Autores: 14
|
| Tipo de documento: | Artigo Científico |
| Fonte: | Polyhedron; v. 282, p. 14-pg., 2025-09-20. |
| Resumo | |
The global burden of cancer continues to grow, and while standard therapies are extensively used, they are often associated with significant side effects. In this study, four novel ruthenium(II) complexes 1-4 with the general formula [Ru(L)(bipy)(dppb)]PF6 were synthesized, in which L represents vanillin-piperidine thiosemicarbazone derivatives. The ligands were derived from the modification of 3-methoxy-4-[2-(piperidine-1-yl)ethoxy]benzaldehyde (VP) with various thiosemicarbazides: hydrogen (L1), methyl (L2), ethyl (L3), and phenyl (L4). The complexes 1-4 were characterized using UV-Vis spectroscopy, FTIR spectroscopy, elemental analysis, molar conductivity, mass spectrometry, cyclic voltammetry (CV), and NMR techniques, including 1H, 13C, 31P{1H}, HSQC, COSY, and DEPTQ. The in vitro cytotoxicity of the complexes was evaluated using the MTT assay against human lung carcinoma (A549), breast adenocarcinoma (MDA-MB-231), and non-tumorigenic lung (MRC-5) and breast (MCF-10 A) cell lines. All complexes demonstrated decreased IC50 values, suggesting enhanced antitumor activity compared to cisplatin. Among them, complex 4 exhibited better activity against MDA-MB-231 cells (IC50 = 0.99 +/- 0.07 mu M; SI = 6.66). Morphological evaluation and clonogenic studies showed that complex 4 alters tumor cell structure and inhibits colony proliferation. DNA binding studies, including UV-Vis titration, competitive binding assays (hoechst 33258 and thiazole orange), circular dichroism, and viscosity measurements, suggested that complex 4 interacts with DNA through a weak binding mode. Human serum albumin (HSA) binding studies revealed moderate, spontaneous interaction driven mainly by hydrophobic forces, while agarose gel electrophoresis confirmed concentration-dependent interaction with pBR322 DNA. Overall findings position complex 4 suggest as a promising candidate for further studies in anticancer therapeutics. (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: | 22/14041-0 - Planejamento e investigação do potencial antitumoral de complexos metálicos contra células metastáticas e/ou quimiorresistentes |
| Beneficiário: | Adelino Vieira de Godoy Netto |
| Modalidade de apoio: | Auxílio à Pesquisa - Regular |