Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes

Autores
Urquiza, Nora María; Islas, María Soledad; Ariza, Santiago T.; Jori, Nadir; Martínez Medina, Juan José; Lavecchia, Martín José; López Tévez, Libertad Leonor; Lezama, Luis; Rojo, Teófilo; Williams, Patricia Ana María; Ferrer, Evelina Gloria
Año de publicación
2015
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
It has been reported that various metal coordination compounds have improved some biological properties. A high activity of acid phosphatase (AcP) is associated to several diseases (osteoporosis, Alzheimer's, prostate cancer, among others) and makes it a target for the development of new potential inhibitors. Anti-thyroid agents have disadvantageous side effects and the scarcity of medicines in this area motivated many researchers to synthesize new ones. Several copper(II) complexes have shown antifungal activities. In this work we presented for a first time the inhibition of AcP and the anti-thyroid activity produced by methimazole-Cu(II) complexes. Cu-Met ([Cu(MeimzH)2(H2O)2](NO3)2·H2O) produces a weak inhibition action while Cu-Met-phen ([Cu(MeimzH)2(phen)(H2O)2]Cl2) shows a strong inhibition effect (IC50 = 300 μM) being more effective than the reported behavior of vanadium complexes. Cu-Met-phen also presented a fairly good anti-thyroid activity with a formation constant value, Kc = 1.02 × 1010 M-1 being 106 times more active than methimazole (Kc = 4.16 × 104 M-1) in opposition to Cu-Met which presented activity (Kc = 9.54 × 103 M-1) but in a lesser extent than that of the free ligand. None of the complexes show antifungal activity except Cu-phen (MIC = 11.71 μg mL-1 on Candida albicans) which was tested for comparison. Besides, albumin interaction experiments denoted high affinity toward the complexes and the calculated binding constants indicate reversible binding to the protein.
Fil: Urquiza, Nora María. Universidad Nacional de Tucumán; Argentina
Fil: Islas, María Soledad. 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: Ariza, Santiago T.. Universidad Nacional de La Plata; Argentina
Fil: Jori, Nadir. Universidad Nacional de La Plata; Argentina
Fil: Martínez Medina, Juan José. Universidad Nacional del Chaco Austral; Argentina
Fil: Lavecchia, Martín José. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; Argentina
Fil: López Tévez, Libertad Leonor. Universidad Nacional del Chaco Austral; Argentina
Fil: Lezama, Luis. Universidad del País Vasco; España
Fil: Rojo, Teófilo. Universidad del País Vasco; España
Fil: Williams, Patricia Ana María. Universidad Nacional de La Plata; Argentina
Fil: Ferrer, Evelina Gloria. Universidad Nacional de La Plata; Argentina
Materia
Methimazole
Phenanthroline
Copper(Ii)
Antifungal Activity
Anti-Thyroid Activity
Bsa Interactions
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/38057
Acceder
id CONICETDig_0bbe8fba101463b839adde3be1c2da5a
oai_identifier_str oai:ri.conicet.gov.ar:11336/38057
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexesUrquiza, Nora MaríaIslas, María SoledadAriza, Santiago T.Jori, NadirMartínez Medina, Juan JoséLavecchia, Martín JoséLópez Tévez, Libertad LeonorLezama, LuisRojo, TeófiloWilliams, Patricia Ana MaríaFerrer, Evelina GloriaMethimazolePhenanthrolineCopper(Ii)Antifungal ActivityAnti-Thyroid ActivityBsa Interactionshttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1It has been reported that various metal coordination compounds have improved some biological properties. A high activity of acid phosphatase (AcP) is associated to several diseases (osteoporosis, Alzheimer's, prostate cancer, among others) and makes it a target for the development of new potential inhibitors. Anti-thyroid agents have disadvantageous side effects and the scarcity of medicines in this area motivated many researchers to synthesize new ones. Several copper(II) complexes have shown antifungal activities. In this work we presented for a first time the inhibition of AcP and the anti-thyroid activity produced by methimazole-Cu(II) complexes. Cu-Met ([Cu(MeimzH)2(H2O)2](NO3)2·H2O) produces a weak inhibition action while Cu-Met-phen ([Cu(MeimzH)2(phen)(H2O)2]Cl2) shows a strong inhibition effect (IC50 = 300 μM) being more effective than the reported behavior of vanadium complexes. Cu-Met-phen also presented a fairly good anti-thyroid activity with a formation constant value, Kc = 1.02 × 1010 M-1 being 106 times more active than methimazole (Kc = 4.16 × 104 M-1) in opposition to Cu-Met which presented activity (Kc = 9.54 × 103 M-1) but in a lesser extent than that of the free ligand. None of the complexes show antifungal activity except Cu-phen (MIC = 11.71 μg mL-1 on Candida albicans) which was tested for comparison. Besides, albumin interaction experiments denoted high affinity toward the complexes and the calculated binding constants indicate reversible binding to the protein.Fil: Urquiza, Nora María. Universidad Nacional de Tucumán; ArgentinaFil: Islas, María Soledad. 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: Ariza, Santiago T.. Universidad Nacional de La Plata; ArgentinaFil: Jori, Nadir. Universidad Nacional de La Plata; ArgentinaFil: Martínez Medina, Juan José. Universidad Nacional del Chaco Austral; ArgentinaFil: Lavecchia, Martín José. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; ArgentinaFil: López Tévez, Libertad Leonor. Universidad Nacional del Chaco Austral; ArgentinaFil: Lezama, Luis. Universidad del País Vasco; EspañaFil: Rojo, Teófilo. Universidad del País Vasco; EspañaFil: Williams, Patricia Ana María. Universidad Nacional de La Plata; ArgentinaFil: Ferrer, Evelina Gloria. Universidad Nacional de La Plata; ArgentinaElsevier Ireland2015-03info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/38057Urquiza, Nora María; Islas, María Soledad; Ariza, Santiago T.; Jori, Nadir; Martínez Medina, Juan José; et al.; Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes; Elsevier Ireland; Chemico-biological Interactions; 229; 3-2015; 64-720009-2797CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0009279715000022info:eu-repo/semantics/altIdentifier/doi/10.1016/j.cbi.2014.12.036info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T11:11:57Zoai:ri.conicet.gov.ar:11336/38057instacron: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:34982025-10-22 11:11:58.193CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
title Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
spellingShingle Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
Urquiza, Nora María
Methimazole
Phenanthroline
Copper(Ii)
Antifungal Activity
Anti-Thyroid Activity
Bsa Interactions
title_short Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
title_full Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
title_fullStr Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
title_full_unstemmed Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
title_sort Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
dc.creator.none.fl_str_mv Urquiza, Nora María
Islas, María Soledad
Ariza, Santiago T.
Jori, Nadir
Martínez Medina, Juan José
Lavecchia, Martín José
López Tévez, Libertad Leonor
Lezama, Luis
Rojo, Teófilo
Williams, Patricia Ana María
Ferrer, Evelina Gloria
author Urquiza, Nora María
author_facet Urquiza, Nora María
Islas, María Soledad
Ariza, Santiago T.
Jori, Nadir
Martínez Medina, Juan José
Lavecchia, Martín José
López Tévez, Libertad Leonor
Lezama, Luis
Rojo, Teófilo
Williams, Patricia Ana María
Ferrer, Evelina Gloria
author_role author
author2 Islas, María Soledad
Ariza, Santiago T.
Jori, Nadir
Martínez Medina, Juan José
Lavecchia, Martín José
López Tévez, Libertad Leonor
Lezama, Luis
Rojo, Teófilo
Williams, Patricia Ana María
Ferrer, Evelina Gloria
author2_role author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Methimazole
Phenanthroline
Copper(Ii)
Antifungal Activity
Anti-Thyroid Activity
Bsa Interactions
topic Methimazole
Phenanthroline
Copper(Ii)
Antifungal Activity
Anti-Thyroid Activity
Bsa Interactions
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv It has been reported that various metal coordination compounds have improved some biological properties. A high activity of acid phosphatase (AcP) is associated to several diseases (osteoporosis, Alzheimer's, prostate cancer, among others) and makes it a target for the development of new potential inhibitors. Anti-thyroid agents have disadvantageous side effects and the scarcity of medicines in this area motivated many researchers to synthesize new ones. Several copper(II) complexes have shown antifungal activities. In this work we presented for a first time the inhibition of AcP and the anti-thyroid activity produced by methimazole-Cu(II) complexes. Cu-Met ([Cu(MeimzH)2(H2O)2](NO3)2·H2O) produces a weak inhibition action while Cu-Met-phen ([Cu(MeimzH)2(phen)(H2O)2]Cl2) shows a strong inhibition effect (IC50 = 300 μM) being more effective than the reported behavior of vanadium complexes. Cu-Met-phen also presented a fairly good anti-thyroid activity with a formation constant value, Kc = 1.02 × 1010 M-1 being 106 times more active than methimazole (Kc = 4.16 × 104 M-1) in opposition to Cu-Met which presented activity (Kc = 9.54 × 103 M-1) but in a lesser extent than that of the free ligand. None of the complexes show antifungal activity except Cu-phen (MIC = 11.71 μg mL-1 on Candida albicans) which was tested for comparison. Besides, albumin interaction experiments denoted high affinity toward the complexes and the calculated binding constants indicate reversible binding to the protein.
Fil: Urquiza, Nora María. Universidad Nacional de Tucumán; Argentina
Fil: Islas, María Soledad. 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: Ariza, Santiago T.. Universidad Nacional de La Plata; Argentina
Fil: Jori, Nadir. Universidad Nacional de La Plata; Argentina
Fil: Martínez Medina, Juan José. Universidad Nacional del Chaco Austral; Argentina
Fil: Lavecchia, Martín José. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Parque Centenario. Instituto de Investigación en Biomedicina de Buenos Aires - Instituto Partner de la Sociedad Max Planck; Argentina
Fil: López Tévez, Libertad Leonor. Universidad Nacional del Chaco Austral; Argentina
Fil: Lezama, Luis. Universidad del País Vasco; España
Fil: Rojo, Teófilo. Universidad del País Vasco; España
Fil: Williams, Patricia Ana María. Universidad Nacional de La Plata; Argentina
Fil: Ferrer, Evelina Gloria. Universidad Nacional de La Plata; Argentina
description It has been reported that various metal coordination compounds have improved some biological properties. A high activity of acid phosphatase (AcP) is associated to several diseases (osteoporosis, Alzheimer's, prostate cancer, among others) and makes it a target for the development of new potential inhibitors. Anti-thyroid agents have disadvantageous side effects and the scarcity of medicines in this area motivated many researchers to synthesize new ones. Several copper(II) complexes have shown antifungal activities. In this work we presented for a first time the inhibition of AcP and the anti-thyroid activity produced by methimazole-Cu(II) complexes. Cu-Met ([Cu(MeimzH)2(H2O)2](NO3)2·H2O) produces a weak inhibition action while Cu-Met-phen ([Cu(MeimzH)2(phen)(H2O)2]Cl2) shows a strong inhibition effect (IC50 = 300 μM) being more effective than the reported behavior of vanadium complexes. Cu-Met-phen also presented a fairly good anti-thyroid activity with a formation constant value, Kc = 1.02 × 1010 M-1 being 106 times more active than methimazole (Kc = 4.16 × 104 M-1) in opposition to Cu-Met which presented activity (Kc = 9.54 × 103 M-1) but in a lesser extent than that of the free ligand. None of the complexes show antifungal activity except Cu-phen (MIC = 11.71 μg mL-1 on Candida albicans) which was tested for comparison. Besides, albumin interaction experiments denoted high affinity toward the complexes and the calculated binding constants indicate reversible binding to the protein.
publishDate 2015
dc.date.none.fl_str_mv 2015-03
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/11336/38057
Urquiza, Nora María; Islas, María Soledad; Ariza, Santiago T.; Jori, Nadir; Martínez Medina, Juan José; et al.; Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes; Elsevier Ireland; Chemico-biological Interactions; 229; 3-2015; 64-72
0009-2797
CONICET Digital
CONICET
url http://hdl.handle.net/11336/38057
identifier_str_mv Urquiza, Nora María; Islas, María Soledad; Ariza, Santiago T.; Jori, Nadir; Martínez Medina, Juan José; et al.; Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes; Elsevier Ireland; Chemico-biological Interactions; 229; 3-2015; 64-72
0009-2797
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0009279715000022
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.cbi.2014.12.036
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
application/pdf
application/pdf
application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier Ireland
publisher.none.fl_str_mv Elsevier Ireland
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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score 13.229304

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