Risedronate metal complexes potentially active against Chagas disease
| Autor: | Mercedes González, Melina Galizzi, Francesco Caruso, Miriam Rossi, Hugo Cerecetto, Dinorah Gambino, Roberto Docampo, Bruno Demoro, Lucía Otero, Diego Benítez, Beatriz S. Parajón-Costa, Jorge Castiglioni |
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| Rok vydání: | 2010 |
| Předmět: |
Chagas disease
Bioquímica RISEDRONATE METAL COMPLEXES Stereochemistry Metal ions in aqueous solution Trypanosoma cruzi Crystal structure Biochemistry Article Inorganic Chemistry Metal chemistry.chemical_compound Farnesyl diphosphate synthase X-Ray Diffraction Coordination Complexes medicine Animals Chagas Disease Risedronate metal complexes biology Ligand CHAGAS DISEASE Otras Ciencias Químicas Ciencias Químicas Etidronic Acid Geranyltranstransferase TRYPANOSOMA CRUZI medicine.disease Phosphonate chemistry Models Chemical visual_art visual_art.visual_art_medium biology.protein Growth inhibition Risedronic Acid CIENCIAS NATURALES Y EXACTAS |
| Zdroj: | Journal of inorganic biochemistry 104 (2010): 1252–1258. doi:10.1016/j.jinorgbio.2010.08.004 info:cnr-pdr/source/autori:Demoro Bruno; Caruso Francesco; Rossi Miriam; Bentez Diego; Gonzalez Mercedes; Cerecetto Hugo; Parajon-Costa Beatriz; Castiglioni Jorge; Galizzi Melina; Docampo Roberto; Otero Luca ; Gambino Dinorah/titolo:Risedronate metal complexes potentially active against Chagas disease/doi:10.1016%2Fj.jinorgbio.2010.08.004/rivista:Journal of inorganic biochemistry/anno:2010/pagina_da:1252/pagina_a:1258/intervallo_pagine:1252–1258/volume:104 |
| ISSN: | 1873-3344 |
| DOI: | 10.1016/j.jinorgbio.2010.08.004 |
| Popis: | 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), [MII(Ris)₂]·4H₂O, where M═Cu, Co, Mn and Ni, and [NiII(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 [CuII(Ris)₂]·4H₂O and [NiII(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. Centro de Química Inorgánica |
| Databáze: | OpenAIRE |
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