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
- Institución
- Consejo Nacional de Investigaciones Científicas y Técnicas
- OAI Identificador
- oai:ri.conicet.gov.ar:11336/38057
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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 Técnicas2025-09-29T09:43:20Zoai: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:34982025-09-29 09:43:20.323CONICET 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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1844613363786579968 |
score |
13.070432 |