Risedronate metal complexes potentially active against Chagas disease
- Autores
- Demoro, Bruno; Caruso, Francesco; Rossi, Miriam; Benítez, Diego; Gonzalez, Mercedes; Cerecetto, Hugo; Parajón Costa, Beatriz Susana; Castiglioni, Jorge; Galizzi. Melina; Docampo, Roberto; Otero, Lucía; Gambino, Dinorah
- Año de publicación
- 2010
- Idioma
- inglés
- Tipo de recurso
- artículo
- Estado
- versión publicada
- Descripción
- 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 Trypanosoma 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.
Fil: Demoro, Bruno. Universidad de la República; Uruguay
Fil: Caruso, Francesco. Istituto Chimica Biomolecolare; Italia
Fil: Rossi, Miriam. Vassar College. Department of Chemistry; Estados Unidos
Fil: Benítez, Diego. Universidad de la República; Uruguay
Fil: Gonzalez, Mercedes. Universidad de la República; Uruguay
Fil: Cerecetto, Hugo. Universidad de la República; Uruguay
Fil: Parajón Costa, Beatriz Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; Argentina
Fil: Castiglioni, Jorge. Universidad de la República; Uruguay
Fil: Galizzi. Melina. University of Georgia; Estados Unidos
Fil: Docampo, Roberto. University of Georgia; Estados Unidos
Fil: Otero, Lucía. Universidad de la República; Uruguay
Fil: Gambino, Dinorah. Universidad de la República; Uruguay - Materia
-
CHAGAS DISEASE
TRYPANOSOMA CRUZI
RISEDRONATE METAL COMPLEXES - Nivel de accesibilidad
- acceso abierto
- Condiciones de uso
- https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
- Repositorio
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/103520
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Risedronate metal complexes potentially active against Chagas diseaseDemoro, BrunoCaruso, FrancescoRossi, MiriamBenítez, DiegoGonzalez, MercedesCerecetto, HugoParajón Costa, Beatriz SusanaCastiglioni, JorgeGalizzi. MelinaDocampo, RobertoOtero, LucíaGambino, DinorahCHAGAS DISEASETRYPANOSOMA CRUZIRISEDRONATE METAL COMPLEXEShttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1In 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 Trypanosoma 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.Fil: Demoro, Bruno. Universidad de la República; UruguayFil: Caruso, Francesco. Istituto Chimica Biomolecolare; ItaliaFil: Rossi, Miriam. Vassar College. Department of Chemistry; Estados UnidosFil: Benítez, Diego. Universidad de la República; UruguayFil: Gonzalez, Mercedes. Universidad de la República; UruguayFil: Cerecetto, Hugo. Universidad de la República; UruguayFil: Parajón Costa, Beatriz Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; ArgentinaFil: Castiglioni, Jorge. Universidad de la República; UruguayFil: Galizzi. Melina. University of Georgia; Estados UnidosFil: Docampo, Roberto. University of Georgia; Estados UnidosFil: Otero, Lucía. Universidad de la República; UruguayFil: Gambino, Dinorah. Universidad de la República; UruguayElsevier Science Inc2010-12info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/103520Demoro, Bruno; Caruso, Francesco; Rossi, Miriam; Benítez, Diego; Gonzalez, Mercedes; et al.; Risedronate metal complexes potentially active against Chagas disease; Elsevier Science Inc; Journal of Inorganic Biochemistry; 104; 12; 12-2010; 1252-12580162-0134CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0162013410001881?via%3Dihubinfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.jinorgbio.2010.08.004info:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5595630/info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-17T10:47:23Zoai:ri.conicet.gov.ar:11336/103520instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-17 10:47:23.402CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse |
dc.title.none.fl_str_mv |
Risedronate metal complexes potentially active against Chagas disease |
title |
Risedronate metal complexes potentially active against Chagas disease |
spellingShingle |
Risedronate metal complexes potentially active against Chagas disease Demoro, Bruno CHAGAS DISEASE TRYPANOSOMA CRUZI RISEDRONATE METAL COMPLEXES |
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 |
dc.creator.none.fl_str_mv |
Demoro, Bruno Caruso, Francesco Rossi, Miriam Benítez, Diego Gonzalez, Mercedes Cerecetto, Hugo Parajón Costa, Beatriz Susana Castiglioni, Jorge Galizzi. Melina Docampo, Roberto Otero, Lucía Gambino, Dinorah |
author |
Demoro, Bruno |
author_facet |
Demoro, Bruno Caruso, Francesco Rossi, Miriam Benítez, Diego Gonzalez, Mercedes Cerecetto, Hugo Parajón Costa, Beatriz Susana Castiglioni, Jorge Galizzi. Melina Docampo, Roberto Otero, Lucía Gambino, Dinorah |
author_role |
author |
author2 |
Caruso, Francesco Rossi, Miriam Benítez, Diego Gonzalez, Mercedes Cerecetto, Hugo Parajón Costa, Beatriz Susana Castiglioni, Jorge Galizzi. Melina Docampo, Roberto Otero, Lucía Gambino, Dinorah |
author2_role |
author author author author author author author author author author author |
dc.subject.none.fl_str_mv |
CHAGAS DISEASE TRYPANOSOMA CRUZI RISEDRONATE METAL COMPLEXES |
topic |
CHAGAS DISEASE TRYPANOSOMA CRUZI RISEDRONATE METAL COMPLEXES |
purl_subject.fl_str_mv |
https://purl.org/becyt/ford/1.4 https://purl.org/becyt/ford/1 |
dc.description.none.fl_txt_mv |
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 Trypanosoma 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. Fil: Demoro, Bruno. Universidad de la República; Uruguay Fil: Caruso, Francesco. Istituto Chimica Biomolecolare; Italia Fil: Rossi, Miriam. Vassar College. Department of Chemistry; Estados Unidos Fil: Benítez, Diego. Universidad de la República; Uruguay Fil: Gonzalez, Mercedes. Universidad de la República; Uruguay Fil: Cerecetto, Hugo. Universidad de la República; Uruguay Fil: Parajón Costa, Beatriz Susana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Centro de Química Inorgánica "Dr. Pedro J. Aymonino". Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Centro de Química Inorgánica "Dr. Pedro J. Aymonino"; Argentina Fil: Castiglioni, Jorge. Universidad de la República; Uruguay Fil: Galizzi. Melina. University of Georgia; Estados Unidos Fil: Docampo, Roberto. University of Georgia; Estados Unidos Fil: Otero, Lucía. Universidad de la República; Uruguay Fil: Gambino, Dinorah. Universidad de la República; Uruguay |
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), [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 Trypanosoma 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. |
publishDate |
2010 |
dc.date.none.fl_str_mv |
2010-12 |
dc.type.none.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion http://purl.org/coar/resource_type/c_6501 info:ar-repo/semantics/articulo |
format |
article |
status_str |
publishedVersion |
dc.identifier.none.fl_str_mv |
http://hdl.handle.net/11336/103520 Demoro, Bruno; Caruso, Francesco; Rossi, Miriam; Benítez, Diego; Gonzalez, Mercedes; et al.; Risedronate metal complexes potentially active against Chagas disease; Elsevier Science Inc; Journal of Inorganic Biochemistry; 104; 12; 12-2010; 1252-1258 0162-0134 CONICET Digital CONICET |
url |
http://hdl.handle.net/11336/103520 |
identifier_str_mv |
Demoro, Bruno; Caruso, Francesco; Rossi, Miriam; Benítez, Diego; Gonzalez, Mercedes; et al.; Risedronate metal complexes potentially active against Chagas disease; Elsevier Science Inc; Journal of Inorganic Biochemistry; 104; 12; 12-2010; 1252-1258 0162-0134 CONICET Digital CONICET |
dc.language.none.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0162013410001881?via%3Dihub info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jinorgbio.2010.08.004 info:eu-repo/semantics/altIdentifier/url/https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5595630/ |
dc.rights.none.fl_str_mv |
info:eu-repo/semantics/openAccess https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
eu_rights_str_mv |
openAccess |
rights_invalid_str_mv |
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/ |
dc.format.none.fl_str_mv |
application/pdf application/pdf application/pdf |
dc.publisher.none.fl_str_mv |
Elsevier Science Inc |
publisher.none.fl_str_mv |
Elsevier Science Inc |
dc.source.none.fl_str_mv |
reponame:CONICET Digital (CONICET) instname:Consejo Nacional de Investigaciones Científicas y Técnicas |
reponame_str |
CONICET Digital (CONICET) |
collection |
CONICET Digital (CONICET) |
instname_str |
Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.name.fl_str_mv |
CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas |
repository.mail.fl_str_mv |
dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar |
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1843606057615622144 |
score |
13.001348 |