Artículos de revistas
Platinum(II) metal complexes as potential anti-Trypanosoma cruzi agents
Fecha
2008-05Registro en:
JOURNAL OF INORGANIC BIOCHEMISTRY, Volume: 102, Issue: 5-6, Pages: 1033-1043, 2008
0162-0134
Autor
Vieites, Marisol
Otero, Lucía
Santos, Diego
Toloza, Jeannette
Figueroa, Roberto
Norambuena, Ester
Olea Azar, Claudio
Aguirre, Gabriela
Cerecetto, Hugo
González, Mercedes
Morello Casté, Antonio
Maya Arango, Juan
Garat, Beatriz
Gambino, Dinorah
Institución
Resumen
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 lMrange 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.