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Heteroleptic oxidovanadium(IV) complexes of 2-hydroxynaphtylaldimine and polypyridyl ligands against Trypanosoma cruzi and prostate cancer cells.
Scalese, Gonzalo; Mosquillo, M Florencia; Rostán, Santiago; Castiglioni, Jorge; Alho, Irina; Pérez, Leticia; Correia, Isabel; Marques, Fernanda; Costa Pessoa, João; Gambino, Dinorah.
Afiliação
  • Scalese G; Química Inorgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay.
  • Mosquillo MF; Laboratorio de Interacciones Moleculares, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
  • Rostán S; Química Inorgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay.
  • Castiglioni J; LAFIDESU, DETEMA, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay.
  • Alho I; Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, A. Professor Egas Moniz, 1649-028 Lisboa, Portugal.
  • Pérez L; Laboratorio de Interacciones Moleculares, Facultad de Ciencias, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.
  • Correia I; Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av Rovisco Pais, 1049-001 Lisboa, Portugal.
  • Marques F; Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, Estrada Nacional 10, 2695-066 Bobadela LRS, Portugal.
  • Costa Pessoa J; Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av Rovisco Pais, 1049-001 Lisboa, Portugal. Electronic address: joao.pessoa@ist.utl.pt.
  • Gambino D; Química Inorgánica, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay. Electronic address: dgambino@fq.edu.uy.
J Inorg Biochem ; 175: 154-166, 2017 10.
Article em En | MEDLINE | ID: mdl-28755573
In Latin America Chagas disease is an endemic illness caused by the parasite Trypanosoma cruzi (T. cruzi), killing more people than any other parasitic disease. Current chemotherapies are old and inadequate, thus the development of efficient ones is urgently needed. Vanadium-based complexes have been shown to be a promising approach both against parasitic diseases and cancer and this study aims to achieve significant advances in the pursue of effective compounds. Heteroleptic vanadium complexes of Schiff bases and polypyridine compounds were prepared and their stability in solution evaluated by EPR (Electronic Paramagnetic Resonance) and NMR spectroscopy. Their in vitro activities were evaluated against T. cruzi and a set of cells lines representative of human cancer conditions, namely ovarian, breast and prostate cancer. In T. cruzi, most of the complexes depicted IC50 values in the low µM range, induced changes of mitochondrial membrane potential and apoptosis. In cancer cells, complexes showed good to moderate activity and in metastatic cells (prostate PC3), some complexes inhibited the migratory ability, this suggesting that they display antimetastatic potential. Interestingly, complex 5 seemed to have a dual effect being the most cytotoxic complex on all cancer cells and also the most active anti-T-cruzi compound of the series. Globally the complexes showed promising anticancer and anti T. cruzi activities and also displayed some characteristics indicating they are worth to be further explored as antimetastatic drugs.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Piridinas / Tripanossomicidas / Trypanosoma cruzi / Vanadatos / Doença de Chagas / Complexos de Coordenação / Antineoplásicos Limite: Humans / Male Idioma: En Revista: J Inorg Biochem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Uruguai País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Neoplasias da Próstata / Piridinas / Tripanossomicidas / Trypanosoma cruzi / Vanadatos / Doença de Chagas / Complexos de Coordenação / Antineoplásicos Limite: Humans / Male Idioma: En Revista: J Inorg Biochem Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Uruguai País de publicação: Estados Unidos