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dc.contributor.author Islas, María Soledad
dc.contributor.author Martínez Medina, Juan José
dc.contributor.author López Tévez, Libertad Leonor
dc.contributor.author Rojo, Teófilo
dc.contributor.author Lezama, Luis
dc.contributor.author Griera Merino, Mercedes
dc.contributor.author Calleros, Laura
dc.contributor.author Cortés, María Alicia
dc.contributor.author Rodriguez Puyol, Manuel
dc.contributor.author Echeverría, Gustavo Alberto
dc.contributor.author Piro, Oscar Enrique
dc.contributor.author Ferrer, Evelina Gloria
dc.contributor.author Williams, Patricia Ana María
dc.date.available 2017-09-11T17:08:16Z
dc.date.issued 2014-05-13
dc.identifier.citation Islas, María Soledad; Martínez Medina, Juan José; López Tévez, Libertad Leonor; Rojo, Teófilo; Lezama, Luis; et al.; Antitumoral, Antihypertensive, Antimicrobial, and Antioxidant Effects of an Octanuclear Copper(II)-Telmisartan Complex with an Hydrophobic Nanometer Hole; American Chemical Society; Inorganic Chemistry; 53; 11; 13-5-2014; 5724-5737
dc.identifier.issn 0020-1669
dc.identifier.uri http://hdl.handle.net/11336/23899
dc.description.abstract A new Cu(II) complex with the antihypertensive drug telmisartan, [Cu8Tlm16].24H2O (CuTlm), was synthesized and characterized by elemental analysis and electronic, FTIR, Raman and EPR spectroscopy. The crystal structure (at 120 K) was solved by X-ray diffraction methods. The octanuclear complex is a hydrate of but otherwise isostructural to the previously reported [Cu8Tlm16] complex. [Cu8Tlm16].24H2O crystallizes in the tetragonal P4/ncc space group with a=b=47.335(1), c=30.894(3) Å, Z=4 molecules per unit cell giving a macro-cyclic ring with a double helical structure. The Cu(II) ions are in a distorted bi-pyramidal environment with a somewhat twisted square basis, cis-coordinated at their core N2O2 basis to two carboxylate oxygen and to two terminal benzimidazole nitrogen atoms. Cu8Tlm16 has a toroidal-like shape with a hydrophobic nanometer hole and their crystal packing defines nano-channels that extend along the crystal c-axis. Several biological activities of the complex and the parent ligand were examined in vitro. The antioxidant measurements indicate that the complex behaves as a superoxide dismutase mimics with improved superoxide scavenger power as compared with native sartan. The capacity of telmisartan and its copper complex to expand human mesangial cells (previously contracted by angiotensin II treatment) is similar to each other. The antihypertensive effect of the compounds is attributed to the strongest binding affinity to angiotensin II type 1 receptor and not to the antioxidant effects. The cytotoxic activity of the complex and that of its components was determined against lung cancer cell line A549 and three prostate cancer cell lines (LNCaP, PC-3 and DU 145). The complex displays some inhibitory effect on the A549 line and a high viability decrease on the LNCaP (androgen-sensitive) line. From flow cytometric analysis it was established an apoptotic mechanism for the latter cell line. Telmisartan and CuTlm show antibacterial and antifungal activities in various strains and CuTlm displays improved activity against the Stafilococcus aureus strain as compared with unbounded copper(II).
dc.format application/pdf
dc.language.iso eng
dc.publisher American Chemical Society
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject X-RAY CRYSTAL STRUCTURE
dc.subject TELMIARTAN
dc.subject OCTANUCLEAR COPPER(II) COMPLEX
dc.subject ROS
dc.subject ANTIHYPERTENSIVE
dc.subject ANTIMICROBIAL
dc.subject CYTOTOXICITY
dc.subject.classification Otras Ciencias Físicas
dc.subject.classification Ciencias Físicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.subject.classification Otras Ciencias Químicas
dc.subject.classification Ciencias Químicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.subject.classification Ética relacionada con Biotecnología Médica
dc.subject.classification Biotecnología de la Salud
dc.subject.classification CIENCIAS MÉDICAS Y DE LA SALUD
dc.title Antitumoral, Antihypertensive, Antimicrobial, and Antioxidant Effects of an Octanuclear Copper(II)-Telmisartan Complex with an Hydrophobic Nanometer Hole
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2017-09-06T19:29:16Z
dc.journal.volume 53
dc.journal.number 11
dc.journal.pagination 5724-5737
dc.journal.pais Estados Unidos
dc.journal.ciudad Washington
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
dc.description.fil Fil: Martínez Medina, Juan José. Universidad Nacional del Chaco Austral; Argentina
dc.description.fil Fil: López Tévez, Libertad Leonor. Universidad Nacional del Chaco Austral; Argentina
dc.description.fil Fil: Rojo, Teófilo. Universidad del País Vasco; España
dc.description.fil Fil: Lezama, Luis. Universidad del País Vasco; España
dc.description.fil Fil: Griera Merino, Mercedes. Universidad de Alcalá; España
dc.description.fil Fil: Calleros, Laura. Universidad de Alcalá; España
dc.description.fil Fil: Cortés, María Alicia. Universidad de Alcalá; España. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.description.fil Fil: Rodriguez Puyol, Manuel. Universidad de Alcalá; España
dc.description.fil Fil: Echeverría, Gustavo Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física La Plata. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física La Plata; Argentina
dc.description.fil Fil: Piro, Oscar Enrique. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física La Plata. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física La Plata; Argentina
dc.description.fil Fil: Ferrer, Evelina Gloria. 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
dc.description.fil Fil: Williams, Patricia Ana María. 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
dc.journal.title Inorganic Chemistry
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/abs/10.1021/ic500483p
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/ic500483p


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info:eu-repo/semantics/restrictedAccess 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)