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Artículo

Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH 2 ) 2 [CuCl 4 ]

Martini, NancyIcon ; Parente, Juliana ElenaIcon ; Toledo, Maria EugeniaIcon ; Escudero, Graciela; Laino, Carlos Horacio; Martínez Medina, Juan JoséIcon ; Echeverría, Gustavo AlbertoIcon ; Piro, Oscar EnriqueIcon ; Lezama, Luis; Williams, Patricia Ana María; Ferrer, Evelina GloriaIcon
Fecha de publicación: 06/2017
Editorial: Elsevier Science Inc
Revista: Journal of Inorganic Biochemistry
ISSN: 0162-0134
e-ISSN: 1873-3344
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:
Otras Ciencias Químicas

Resumen

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 pseudo-first 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).
Palabras clave: Drug Design , X-Ray Crystal Structure , Pharmacological Activities , Bioavailability
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/41068
URL: https://www.sciencedirect.com/science/article/pii/S0162013417300685
DOI: https://doi.org/10.1016/j.jinorgbio.2017.05.012
Colecciones
Articulos(CCT - NORDESTE)
Articulos de CTRO.CIENTIFICO TECNOL.CONICET - NORDESTE
Articulos(CEQUINOR)
Articulos de CENTRO DE QUIMICA INORGANICA "DR. PEDRO J. AYMONINO"
Articulos(IFLP)
Articulos de INST.DE FISICA LA PLATA
Citación
Martini, Nancy; Parente, Juliana Elena; Toledo, Maria Eugenia; Escudero, Graciela; Laino, Carlos Horacio; et al.; Evidence of promising biological-pharmacological activities of the sertraline-based copper complex: (SerH 2 ) 2 [CuCl 4 ]; Elsevier Science Inc; Journal of Inorganic Biochemistry; 174; 6-2017; 76-89
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