Platinum(II) metal complexes as potential anti-Trypanosoma cruzi agents.
J Inorg Biochem
; 102(5-6): 1033-43, 2008.
Article
em En
| MEDLINE
| ID: mdl-18226837
ABSTRACT
In the search for new therapeutic tools against Chagas' disease (American Trypanosomiasis) two series of new platinum(II) complexes with bioactive 5-nitrofuryl containing thiosemicarbazones as ligands were synthesized, characterized and in vitro evaluated. Most of the complexes showed IC50 values in the muM range against two different strains of Trypanosoma cruzi, causative agent of the disease, being as active as the anti-trypanosomal drug Nifurtimox. In particular, the coordination of L3 (4-ethyl-1-(5-nitrofurfurylidene)thiosemicarbazide) to Pt(II) forming [Pt(L3)2] lead to almost a five-fold activity increase in respect to the free ligand. Trying to get an insight into the trypanocidal mechanism of action of these compounds, DNA and redox metabolism (intra-parasite free radical production) were evaluated as potential parasite targets. Results suggest that the complexes could inhibit parasite growth through a dual mechanism of action involving production of toxic free radicals by bioreduction and DNA interaction.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos Organoplatínicos
/
Tripanossomicidas
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Trypanosoma cruzi
Limite:
Animals
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article