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
- Institución
- Comisión de Investigaciones Científicas de la Provincia de Buenos Aires
- OAI Identificador
- oai:digital.cic.gba.gob.ar:11746/8102
Ver los metadatos del registro completo
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oai:digital.cic.gba.gob.ar:11746/8102 |
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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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1844618588724396032 |
score |
13.070432 |