Risedronate metal complexes potentially active against Chagas disease

In the search for new metal-based drugs for the treatment of Chagas disease, the most widespread Latin American parasitic disease, novel complexes of the bioactive ligand risedronate (Ris, (1-hydroxy-1-phosphono-2-pyridin-3-yl-ethyl)phosphonate), [M<sup>II</sup>(Ris)₂]·4H₂O, where M═Cu,...

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Detalles Bibliográficos
Autores principales: Demoro, Bruno, Caruso, Francesco, Rossi, Miriam, Benítez, Diego, González, Mercedes, Cerecetto, Hugo, Parajón Costa, Beatriz Susana, Castiglioni, Jorge, Galizzi, Melina, Docampo, Roberto, Otero, Lucía, Gambino, Dinorah
Formato: Articulo Preprint
Lenguaje:Inglés
Publicado: 2010
Materias:
Bioquímica
Chagas disease
Trypanosoma cruzi
Risedronate metal complexes
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/127953
Aporte de:
SEDICI (UNLP) de Universidad Nacional de La Plata
id I19-R120-10915-127953
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Bioquímica
Chagas disease
Trypanosoma cruzi
Risedronate metal complexes
spellingShingle Bioquímica
Chagas disease
Trypanosoma cruzi
Risedronate metal complexes
Demoro, Bruno
Caruso, Francesco
Rossi, Miriam
Benítez, Diego
González, Mercedes
Cerecetto, Hugo
Parajón Costa, Beatriz Susana
Castiglioni, Jorge
Galizzi, Melina
Docampo, Roberto
Otero, Lucía
Gambino, Dinorah
Risedronate metal complexes potentially active against Chagas disease
topic_facet Bioquímica
Chagas disease
Trypanosoma cruzi
Risedronate metal complexes
description In the search for new metal-based drugs for the treatment of Chagas disease, the most widespread Latin American parasitic disease, novel complexes of the bioactive ligand risedronate (Ris, (1-hydroxy-1-phosphono-2-pyridin-3-yl-ethyl)phosphonate), [M<sup>II</sup>(Ris)₂]·4H₂O, where M═Cu, Co, Mn and Ni, and [Ni<sup>II</sup>(Ris)₂(H₂O)2]·H₂O were synthesized and characterized by using analytical measurements, thermogravimetric analyses, cyclic voltammetry and infrared and Raman spectroscopies. Crystal structures of [Cu<sup>II</sup>(Ris)₂]·4H₂O and [Ni<sup>II</sup>(Ris)₂(H₂O)₂]·H₂O were solved by single crystal X-ray diffraction methods. The complexes, as well as the free ligand, were evaluated in vitro against epimastigotes and intracellular amastigotes of the parasite Trypanosoma cruzi, causative agent of Chagas disease. Results demonstrated that the coordination of risedronate to different metal ions improved the antiproliferative effect against T. cruzi, exhibiting growth inhibition values against the intracellular amastigotes ranging the low micromolar levels. In addition, this strong activity could be related to high inhibition of farnesyl diphosphate synthase enzyme. On the other hand, protein interaction studies showed that all the complexes strongly interact with albumin thus providing a suitable means of transporting them to tissues in vivo.
format Articulo
Preprint
author Demoro, Bruno
Caruso, Francesco
Rossi, Miriam
Benítez, Diego
González, Mercedes
Cerecetto, Hugo
Parajón Costa, Beatriz Susana
Castiglioni, Jorge
Galizzi, Melina
Docampo, Roberto
Otero, Lucía
Gambino, Dinorah
author_facet Demoro, Bruno
Caruso, Francesco
Rossi, Miriam
Benítez, Diego
González, Mercedes
Cerecetto, Hugo
Parajón Costa, Beatriz Susana
Castiglioni, Jorge
Galizzi, Melina
Docampo, Roberto
Otero, Lucía
Gambino, Dinorah
author_sort Demoro, Bruno
title Risedronate metal complexes potentially active against Chagas disease
title_short Risedronate metal complexes potentially active against Chagas disease
title_full Risedronate metal complexes potentially active against Chagas disease
title_fullStr Risedronate metal complexes potentially active against Chagas disease
title_full_unstemmed Risedronate metal complexes potentially active against Chagas disease
title_sort risedronate metal complexes potentially active against chagas disease
publishDate 2010
url http://sedici.unlp.edu.ar/handle/10915/127953
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