Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]

Autores
Martini, Nancy; Parente, Juliana Elena; Toledo, María Eugenia; Escudero, Graciela E.; Laino, Carlos; Martínez Medina, Juan José; Echeverría, Gustavo A.; Piro, Oscar E.; Lezama, Luis; Williams, Patricia Ana María; Ferrer, Evelina G.
Año de publicación
2017
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
In the current study the ability of copper complex to exert multiple biological activities is combined with the pharmacological action of sertraline (SerH2Cl, antidepressant drug). The hydrated and anhydrous forms of the tetrachlorocuprate(II) salts, namely (SerH2)2[CuCl4]·½H2O and (SerH2)2[CuCl4], were synthesized and characterized by physicochemical methods. The crystal structures were determined by X-ray diffraction methods. The hydrate complex crystallizes in the monoclinic P21 space group with a =8.0807(2) Å, b =36.2781(8) Å, c =12.6576(3) Å, β =95.665(2)°, and Z =4 molecules per unit cell and the un-hydrate in P21 with a =13.8727(6) Å, b =7.5090(3) Å, c= 18.618(1) Å, β =104.563(6)°, and Z =2. It has been suggested that Cu(II) ions might be critical in the development of mood disorders, showed potent biocidal activity, and also acted as analgesic adjuvant. To improve sertraline efficiency, the antidepressant and analgesic activities of the complex have been assessed in rats denoting a marked synergistic effect. Antithyroid and antimicrobial activities were also evaluated. Because depressive disorders and hyperthyroidism diseases led to an oxidative stress state, antioxidant capability has also been tested. The complex behaved as a good superoxide radical scavenger (IC50=6.3 × 10−6 M). The ability of the complex to act as bromoperoxidase mimic was assessed. A pseudofirst order constant of k = 0.157 ± 0.007 min−1 has been determined. The complex evidences promising biological-pharmacological activities and the albumin binding studies showed a Kb of 2.90 ×103 M−1 showing an improvement in the uptake of sertraline by albumin at 8 h incubation (time required for effective interaction of sertraline with the protein).
Materia
Ciencias Químicas
Drug design
X-ray crystal structure
Pharmacological activities
Bioavailability
Nivel de accesibilidad
acceso abierto
Condiciones de uso
http://creativecommons.org/licenses/by-nc-nd/4.0/
Repositorio
CIC Digital (CICBA)
Institución
Comisión de Investigaciones Científicas de la Provincia de Buenos Aires
OAI Identificador
oai:digital.cic.gba.gob.ar:11746/8102

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oai_identifier_str oai:digital.cic.gba.gob.ar:11746/8102
network_acronym_str CICBA
repository_id_str 9441
network_name_str CIC Digital (CICBA)
spelling Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]Martini, NancyParente, Juliana ElenaToledo, María EugeniaEscudero, Graciela E.Laino, CarlosMartínez Medina, Juan JoséEcheverría, Gustavo A.Piro, Oscar E.Lezama, LuisWilliams, Patricia Ana MaríaFerrer, Evelina G.Ciencias QuímicasDrug designX-ray crystal structurePharmacological activitiesBioavailabilityIn the current study the ability of copper complex to exert multiple biological activities is combined with the pharmacological action of sertraline (SerH2Cl, antidepressant drug). The hydrated and anhydrous forms of the tetrachlorocuprate(II) salts, namely (SerH2)2[CuCl4]·½H2O and (SerH2)2[CuCl4], were synthesized and characterized by physicochemical methods. The crystal structures were determined by X-ray diffraction methods. The hydrate complex crystallizes in the monoclinic P21 space group with a =8.0807(2) Å, b =36.2781(8) Å, c =12.6576(3) Å, β =95.665(2)°, and Z =4 molecules per unit cell and the un-hydrate in P21 with a =13.8727(6) Å, b =7.5090(3) Å, c= 18.618(1) Å, β =104.563(6)°, and Z =2. It has been suggested that Cu(II) ions might be critical in the development of mood disorders, showed potent biocidal activity, and also acted as analgesic adjuvant. To improve sertraline efficiency, the antidepressant and analgesic activities of the complex have been assessed in rats denoting a marked synergistic effect. Antithyroid and antimicrobial activities were also evaluated. Because depressive disorders and hyperthyroidism diseases led to an oxidative stress state, antioxidant capability has also been tested. The complex behaved as a good superoxide radical scavenger (IC50=6.3 × 10−6 M). The ability of the complex to act as bromoperoxidase mimic was assessed. A pseudofirst order constant of k = 0.157 ± 0.007 min−1 has been determined. The complex evidences promising biological-pharmacological activities and the albumin binding studies showed a Kb of 2.90 ×103 M−1 showing an improvement in the uptake of sertraline by albumin at 8 h incubation (time required for effective interaction of sertraline with the protein).Elsevier2017-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfhttps://digital.cic.gba.gob.ar/handle/11746/8102enginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.jinorgbio.2017.05.012info:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-nd/4.0/reponame:CIC Digital (CICBA)instname:Comisión de Investigaciones Científicas de la Provincia de Buenos Airesinstacron:CICBA2025-09-29T13:39:57Zoai:digital.cic.gba.gob.ar:11746/8102Institucionalhttp://digital.cic.gba.gob.arOrganismo científico-tecnológicoNo correspondehttp://digital.cic.gba.gob.ar/oai/snrdmarisa.degiusti@sedici.unlp.edu.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:94412025-09-29 13:39:57.383CIC Digital (CICBA) - Comisión de Investigaciones Científicas de la Provincia de Buenos Airesfalse
dc.title.none.fl_str_mv Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
title Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
spellingShingle Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
Martini, Nancy
Ciencias Químicas
Drug design
X-ray crystal structure
Pharmacological activities
Bioavailability
title_short Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
title_full Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
title_fullStr Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
title_full_unstemmed Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
title_sort Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH2)2[CuCl4]
dc.creator.none.fl_str_mv Martini, Nancy
Parente, Juliana Elena
Toledo, María Eugenia
Escudero, Graciela E.
Laino, Carlos
Martínez Medina, Juan José
Echeverría, Gustavo A.
Piro, Oscar E.
Lezama, Luis
Williams, Patricia Ana María
Ferrer, Evelina G.
author Martini, Nancy
author_facet Martini, Nancy
Parente, Juliana Elena
Toledo, María Eugenia
Escudero, Graciela E.
Laino, Carlos
Martínez Medina, Juan José
Echeverría, Gustavo A.
Piro, Oscar E.
Lezama, Luis
Williams, Patricia Ana María
Ferrer, Evelina G.
author_role author
author2 Parente, Juliana Elena
Toledo, María Eugenia
Escudero, Graciela E.
Laino, Carlos
Martínez Medina, Juan José
Echeverría, Gustavo A.
Piro, Oscar E.
Lezama, Luis
Williams, Patricia Ana María
Ferrer, Evelina G.
author2_role author
author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv Ciencias Químicas
Drug design
X-ray crystal structure
Pharmacological activities
Bioavailability
topic Ciencias Químicas
Drug design
X-ray crystal structure
Pharmacological activities
Bioavailability
dc.description.none.fl_txt_mv In the current study the ability of copper complex to exert multiple biological activities is combined with the pharmacological action of sertraline (SerH2Cl, antidepressant drug). The hydrated and anhydrous forms of the tetrachlorocuprate(II) salts, namely (SerH2)2[CuCl4]·½H2O and (SerH2)2[CuCl4], were synthesized and characterized by physicochemical methods. The crystal structures were determined by X-ray diffraction methods. The hydrate complex crystallizes in the monoclinic P21 space group with a =8.0807(2) Å, b =36.2781(8) Å, c =12.6576(3) Å, β =95.665(2)°, and Z =4 molecules per unit cell and the un-hydrate in P21 with a =13.8727(6) Å, b =7.5090(3) Å, c= 18.618(1) Å, β =104.563(6)°, and Z =2. It has been suggested that Cu(II) ions might be critical in the development of mood disorders, showed potent biocidal activity, and also acted as analgesic adjuvant. To improve sertraline efficiency, the antidepressant and analgesic activities of the complex have been assessed in rats denoting a marked synergistic effect. Antithyroid and antimicrobial activities were also evaluated. Because depressive disorders and hyperthyroidism diseases led to an oxidative stress state, antioxidant capability has also been tested. The complex behaved as a good superoxide radical scavenger (IC50=6.3 × 10−6 M). The ability of the complex to act as bromoperoxidase mimic was assessed. A pseudofirst order constant of k = 0.157 ± 0.007 min−1 has been determined. The complex evidences promising biological-pharmacological activities and the albumin binding studies showed a Kb of 2.90 ×103 M−1 showing an improvement in the uptake of sertraline by albumin at 8 h incubation (time required for effective interaction of sertraline with the protein).
description In the current study the ability of copper complex to exert multiple biological activities is combined with the pharmacological action of sertraline (SerH2Cl, antidepressant drug). The hydrated and anhydrous forms of the tetrachlorocuprate(II) salts, namely (SerH2)2[CuCl4]·½H2O and (SerH2)2[CuCl4], were synthesized and characterized by physicochemical methods. The crystal structures were determined by X-ray diffraction methods. The hydrate complex crystallizes in the monoclinic P21 space group with a =8.0807(2) Å, b =36.2781(8) Å, c =12.6576(3) Å, β =95.665(2)°, and Z =4 molecules per unit cell and the un-hydrate in P21 with a =13.8727(6) Å, b =7.5090(3) Å, c= 18.618(1) Å, β =104.563(6)°, and Z =2. It has been suggested that Cu(II) ions might be critical in the development of mood disorders, showed potent biocidal activity, and also acted as analgesic adjuvant. To improve sertraline efficiency, the antidepressant and analgesic activities of the complex have been assessed in rats denoting a marked synergistic effect. Antithyroid and antimicrobial activities were also evaluated. Because depressive disorders and hyperthyroidism diseases led to an oxidative stress state, antioxidant capability has also been tested. The complex behaved as a good superoxide radical scavenger (IC50=6.3 × 10−6 M). The ability of the complex to act as bromoperoxidase mimic was assessed. A pseudofirst order constant of k = 0.157 ± 0.007 min−1 has been determined. The complex evidences promising biological-pharmacological activities and the albumin binding studies showed a Kb of 2.90 ×103 M−1 showing an improvement in the uptake of sertraline by albumin at 8 h incubation (time required for effective interaction of sertraline with the protein).
publishDate 2017
dc.date.none.fl_str_mv 2017-09
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 https://digital.cic.gba.gob.ar/handle/11746/8102
url https://digital.cic.gba.gob.ar/handle/11746/8102
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.jinorgbio.2017.05.012
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
rights_invalid_str_mv http://creativecommons.org/licenses/by-nc-nd/4.0/
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:CIC Digital (CICBA)
instname:Comisión de Investigaciones Científicas de la Provincia de Buenos Aires
instacron:CICBA
reponame_str CIC Digital (CICBA)
collection CIC Digital (CICBA)
instname_str Comisión de Investigaciones Científicas de la Provincia de Buenos Aires
instacron_str CICBA
institution CICBA
repository.name.fl_str_mv CIC Digital (CICBA) - Comisión de Investigaciones Científicas de la Provincia de Buenos Aires
repository.mail.fl_str_mv marisa.degiusti@sedici.unlp.edu.ar
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