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dc.contributor.author
Urquiza, Nora María
dc.contributor.author
Islas, María Soledad
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Ariza, Santiago T.
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Jori, Nadir
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Martínez Medina, Juan José
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Lavecchia, Martín José
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López Tévez, Libertad Leonor
dc.contributor.author
Lezama, Luis
dc.contributor.author
Rojo, Teófilo
dc.contributor.author
Williams, Patricia Ana María
dc.contributor.author
Ferrer, Evelina Gloria
dc.date.available
2018-03-06T20:14:47Z
dc.date.issued
2015-03
dc.identifier.citation
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
dc.identifier.issn
0009-2797
dc.identifier.uri
http://hdl.handle.net/11336/38057
dc.description.abstract
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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier Ireland
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
Methimazole
dc.subject
Phenanthroline
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Copper(Ii)
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Antifungal Activity
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Anti-Thyroid Activity
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Bsa Interactions
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Otras Ciencias Químicas
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Ciencias Químicas
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CIENCIAS NATURALES Y EXACTAS
dc.title
Anti-thyroid and antifungal activities, BSA interaction and acid phosphatase inhibition of methimazole copper(II) complexes
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2018-02-28T14:12:52Z
dc.journal.volume
229
dc.journal.pagination
64-72
dc.journal.pais
Irlanda
dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Urquiza, Nora María. Universidad Nacional de Tucumán; Argentina
dc.description.fil
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
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Fil: Ariza, Santiago T.. Universidad Nacional de La Plata; Argentina
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Fil: Jori, Nadir. Universidad Nacional de La Plata; Argentina
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Fil: Martínez Medina, Juan José. Universidad Nacional del Chaco Austral; Argentina
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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
dc.description.fil
Fil: López Tévez, Libertad Leonor. Universidad Nacional del Chaco Austral; Argentina
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Fil: Lezama, Luis. Universidad del País Vasco; España
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Fil: Rojo, Teófilo. Universidad del País Vasco; España
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Fil: Williams, Patricia Ana María. Universidad Nacional de La Plata; Argentina
dc.description.fil
Fil: Ferrer, Evelina Gloria. Universidad Nacional de La Plata; Argentina
dc.journal.title
Chemico-biological Interactions
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0009279715000022
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.cbi.2014.12.036
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