Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano

La resistencia a los antimicrobianos (RAM) es una de las diez principales amenazas para la salud pública reportadas por la Organización Mundial de la Salud (OMS). Una de las causas del creciente problema de la RAM es la falta de nuevas terapias y/o agentes de tratamiento; en consecuencia, muchas enf...

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Autores:
Pineda Castañeda, Héctor Manuel
Tipo de recurso:
Doctoral thesis
Fecha de publicación:
2023
Institución:
Universidad Nacional de Colombia
Repositorio:
Universidad Nacional de Colombia
Idioma:
spa
OAI Identifier:
oai:repositorio.unal.edu.co:unal/85642
Acceso en línea:
https://repositorio.unal.edu.co/handle/unal/85642
https://repositorio.unal.edu.co/
Palabra clave:
540 - Química y ciencias afines
Programas de Optimización del Uso de los Antimicrobianos
Antiinfecciosos
Antimicrobial Stewardship
Anti-Infective Agents
Dendrimeros
Péptido
Resorcinareno
Péptidos Antimicrobianos
Química click
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openAccess
License
Reconocimiento 4.0 Internacional
id UNACIONAL2_2864790cd5fa417df0d5a0a03cfaf6ba
oai_identifier_str oai:repositorio.unal.edu.co:unal/85642
network_acronym_str UNACIONAL2
network_name_str Universidad Nacional de Colombia
repository_id_str
dc.title.spa.fl_str_mv Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
dc.title.translated.eng.fl_str_mv Peptide-resorcinarene dendrimers: (i) obtaining by azide/alkyne cycloaddition reaction and (ii) evaluation of their antibacterial potential
title Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
spellingShingle Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
540 - Química y ciencias afines
Programas de Optimización del Uso de los Antimicrobianos
Antiinfecciosos
Antimicrobial Stewardship
Anti-Infective Agents
Dendrimeros
Péptido
Resorcinareno
Péptidos Antimicrobianos
Química click
title_short Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
title_full Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
title_fullStr Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
title_full_unstemmed Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
title_sort Dendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacteriano
dc.creator.fl_str_mv Pineda Castañeda, Héctor Manuel
dc.contributor.advisor.none.fl_str_mv Maldona Villamil, Mauricio
Rivera Monroy, Zuly Jenny
dc.contributor.author.none.fl_str_mv Pineda Castañeda, Héctor Manuel
dc.contributor.researchgroup.spa.fl_str_mv Síntesis y Aplicación de Moléculas Peptídicas
Aplicaciones Analíticas de Compuestos Orgánicos (Aaco)
dc.contributor.orcid.spa.fl_str_mv 0000-0002-9081-0546
dc.contributor.cvlac.spa.fl_str_mv https://scienti.minciencias.gov.co/cvlac/visualizador/generarCurriculoCv.do?cod_rh=0000073189
dc.contributor.scopus.spa.fl_str_mv https://www.scopus.com/authid/detail.uri?authorId=57208139842
dc.contributor.researchgate.spa.fl_str_mv https://www.researchgate.net/profile/Hector-Pineda-Castaneda
dc.contributor.googlescholar.spa.fl_str_mv https://scholar.google.com/citations?user=Wu60Xw0AAAAJ&hl=es&authuser=3
dc.subject.ddc.spa.fl_str_mv 540 - Química y ciencias afines
topic 540 - Química y ciencias afines
Programas de Optimización del Uso de los Antimicrobianos
Antiinfecciosos
Antimicrobial Stewardship
Anti-Infective Agents
Dendrimeros
Péptido
Resorcinareno
Péptidos Antimicrobianos
Química click
dc.subject.decs.spa.fl_str_mv Programas de Optimización del Uso de los Antimicrobianos
Antiinfecciosos
dc.subject.decs.eng.fl_str_mv Antimicrobial Stewardship
Anti-Infective Agents
dc.subject.proposal.spa.fl_str_mv Dendrimeros
Péptido
Resorcinareno
Péptidos Antimicrobianos
Química click
description La resistencia a los antimicrobianos (RAM) es una de las diez principales amenazas para la salud pública reportadas por la Organización Mundial de la Salud (OMS). Una de las causas del creciente problema de la RAM es la falta de nuevas terapias y/o agentes de tratamiento; en consecuencia, muchas enfermedades infecciosas podrían volverse incontrolables. La necesidad de descubrir nuevos agentes antimicrobianos, que sean alternativos a los existentes, y que permitan mitigar este problema, se ha incrementado debido a la rápida y global expansión de la RAM. En este contexto, se han propuesto como alternativas para combatir la RAM tanto los péptidos antimicrobianos (PAMs) como los dendrímeros que presentan múltiples copias de compuestos antibacterianos en su estructura. Los dendrímeros han exhibido propiedades antifúngicas y antibacterianas y también se han utilizado en terapias antiinflamatorias, antineoplásicas y cardiovasculares y son útiles en sistemas de administración de fármacos y genes. En este trabajo se propuso obtener dendrímeros que presenten cuatro copias de secuencias de PAMs. Específicamente, (i) se exploró la síntesis, purificación y caracterización de dendrímeros de péptido-resorcinareno derivados de las secuencias LfcinB (20-25): RRWQWR y BF (32-35): RLLR, y (ii) la actividad antimicrobiana y citotóxica de estos dendrímeros. Se establecieron las rutas de síntesis que permitieron obtener: a) alquino-resorcinarenos y b) péptidos funcionalizados con el grupo azida; los cuales se usaron para generar c) dendrímeros de péptido-resorcinareno mediante química click de cicloadición de azida-alquino CuAAC. Finalmente, se evaluó la actividad antimicrobiana y citotóxica de los dendrímeros obtenidos frente a cepas de referencia y aislados clínicos. Estos resultados permitieron la identificación de moléculas antimicrobianas prometedoras que pueden conducir a avances en el desarrollo de nuevos agentes terapéuticos. (Texto tomado de la fuente)
publishDate 2023
dc.date.issued.none.fl_str_mv 2023
dc.date.accessioned.none.fl_str_mv 2024-02-07T13:53:46Z
dc.date.available.none.fl_str_mv 2024-02-07T13:53:46Z
dc.type.spa.fl_str_mv Trabajo de grado - Doctorado
dc.type.driver.spa.fl_str_mv info:eu-repo/semantics/doctoralThesis
dc.type.version.spa.fl_str_mv info:eu-repo/semantics/acceptedVersion
dc.type.coar.spa.fl_str_mv http://purl.org/coar/resource_type/c_db06
dc.type.content.spa.fl_str_mv DataPaper
dc.type.redcol.spa.fl_str_mv http://purl.org/redcol/resource_type/TD
format http://purl.org/coar/resource_type/c_db06
status_str acceptedVersion
dc.identifier.uri.none.fl_str_mv https://repositorio.unal.edu.co/handle/unal/85642
dc.identifier.instname.spa.fl_str_mv Universidad Nacional de Colombia
dc.identifier.reponame.spa.fl_str_mv Repositorio Institucional Universidad Nacional de Colombia
dc.identifier.repourl.spa.fl_str_mv https://repositorio.unal.edu.co/
url https://repositorio.unal.edu.co/handle/unal/85642
https://repositorio.unal.edu.co/
identifier_str_mv Universidad Nacional de Colombia
Repositorio Institucional Universidad Nacional de Colombia
dc.language.iso.spa.fl_str_mv spa
language spa
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spelling Reconocimiento 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/info:eu-repo/semantics/openAccesshttp://purl.org/coar/access_right/c_abf2Maldona Villamil, Mauricio22af21f285c3f5f3c3e580fae6982abcRivera Monroy, Zuly Jennybcc909fcc85ff0efa659b7aaca42b3cbPineda Castañeda, Héctor Manuel94dc1b0c9bf5fa93da8185efbe9ce789Síntesis y Aplicación de Moléculas PeptídicasAplicaciones Analíticas de Compuestos Orgánicos (Aaco)0000-0002-9081-0546https://scienti.minciencias.gov.co/cvlac/visualizador/generarCurriculoCv.do?cod_rh=0000073189https://www.scopus.com/authid/detail.uri?authorId=57208139842https://www.researchgate.net/profile/Hector-Pineda-Castanedahttps://scholar.google.com/citations?user=Wu60Xw0AAAAJ&hl=es&authuser=32024-02-07T13:53:46Z2024-02-07T13:53:46Z2023https://repositorio.unal.edu.co/handle/unal/85642Universidad Nacional de ColombiaRepositorio Institucional Universidad Nacional de Colombiahttps://repositorio.unal.edu.co/La resistencia a los antimicrobianos (RAM) es una de las diez principales amenazas para la salud pública reportadas por la Organización Mundial de la Salud (OMS). Una de las causas del creciente problema de la RAM es la falta de nuevas terapias y/o agentes de tratamiento; en consecuencia, muchas enfermedades infecciosas podrían volverse incontrolables. La necesidad de descubrir nuevos agentes antimicrobianos, que sean alternativos a los existentes, y que permitan mitigar este problema, se ha incrementado debido a la rápida y global expansión de la RAM. En este contexto, se han propuesto como alternativas para combatir la RAM tanto los péptidos antimicrobianos (PAMs) como los dendrímeros que presentan múltiples copias de compuestos antibacterianos en su estructura. Los dendrímeros han exhibido propiedades antifúngicas y antibacterianas y también se han utilizado en terapias antiinflamatorias, antineoplásicas y cardiovasculares y son útiles en sistemas de administración de fármacos y genes. En este trabajo se propuso obtener dendrímeros que presenten cuatro copias de secuencias de PAMs. Específicamente, (i) se exploró la síntesis, purificación y caracterización de dendrímeros de péptido-resorcinareno derivados de las secuencias LfcinB (20-25): RRWQWR y BF (32-35): RLLR, y (ii) la actividad antimicrobiana y citotóxica de estos dendrímeros. Se establecieron las rutas de síntesis que permitieron obtener: a) alquino-resorcinarenos y b) péptidos funcionalizados con el grupo azida; los cuales se usaron para generar c) dendrímeros de péptido-resorcinareno mediante química click de cicloadición de azida-alquino CuAAC. Finalmente, se evaluó la actividad antimicrobiana y citotóxica de los dendrímeros obtenidos frente a cepas de referencia y aislados clínicos. Estos resultados permitieron la identificación de moléculas antimicrobianas prometedoras que pueden conducir a avances en el desarrollo de nuevos agentes terapéuticos. (Texto tomado de la fuente)Antimicrobial resistance (AMR) is one of the top ten threats to public health reported by the World Health Organization (WHO). One of the causes of the growing AMR problem is the lack of new therapies and/or treatment agents; consequently, many infectious diseases could become uncontrollable. The need to discover new antimicrobial agents, which are alternatives to the existing ones, and which allow mitigating this problem, has increased due to the rapid and global expansion of AMR. In this context, both antimicrobial peptides (AMPs) and dendrimers that present multiple copies of antibacterial compounds in their structure have been proposed as alternatives to combat AMR. Dendrimers have exhibited antifungal and antibacterial properties and have also been used in anti-inflammatory, antineoplastic and cardiovascular therapies and are useful in drug and gene delivery systems. In this work, it was proposed to obtain dendrimers that present four copies of AMPs sequences. Specifically, (i) the synthesis, purification, and characterization of peptide-resorcinarene dendrimers derived from the sequences LfcinB (20-25): RRWQWR and BF (32-35): RLLR, and (ii) the antimicrobial and cytotoxic activity were explored. of these dendrimers. The synthesis routes that allowed obtaining: a) alkyne-resorcinarenes and b) peptides functionalized with the azide group were established, which were used to generate c) peptide-resorcinarene dendrimers by azide-alkyne cycloaddition (CuAAC) click chemistry. Finally, the antimicrobial and cytotoxic activity of the dendrimers obtained was evaluated against reference strains and clinical isolates. These results allowed the identification of promising antimicrobial molecules that may lead to breakthroughs in the development of new therapeutic agents.DoctoradoDoctor en Ciencias - Química269 páginasapplication/pdfspaUniversidad Nacional de ColombiaBogotá - Ciencias - Doctorado en Ciencias - QuímicaFacultad de CienciasBogotá, ColombiaUniversidad Nacional de Colombia - Sede Bogotá540 - Química y ciencias afinesProgramas de Optimización del Uso de los AntimicrobianosAntiinfecciososAntimicrobial StewardshipAnti-Infective AgentsDendrimerosPéptidoResorcinarenoPéptidos AntimicrobianosQuímica clickDendrímeros péptido-resorcinareno: (i) obtención mediante reacción de cicloadición azida/alquino y (ii) evaluación de su potencial antibacterianoPeptide-resorcinarene dendrimers: (i) obtaining by azide/alkyne cycloaddition reaction and (ii) evaluation of their antibacterial potentialTrabajo de grado - Doctoradoinfo:eu-repo/semantics/doctoralThesisinfo:eu-repo/semantics/acceptedVersionhttp://purl.org/coar/resource_type/c_db06DataPaperhttp://purl.org/redcol/resource_type/TDJ. 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Guerra et al., “The tetrameric peptide LfcinB (20-25)4 derived from bovine lactoferricin induces apoptosis in the MCF-7 breast cancer cell line,” RSC Adv, vol. 9, no. 36, pp. 20497–20504, 2019, doi: 10.1039/c9ra04145aDiseño y obtención de nuevos agentes antibacterianos basados en dendrímeros péptido-resorcinareno: Una alternativa para combatir la resistencia bacterianaMincienciasInvestigadoresORIGINAL1016063614.2023.pdf1016063614.2023.pdfTesis de Doctorado en Ciencias - Químicaapplication/pdf49940176https://repositorio.unal.edu.co/bitstream/unal/85642/6/1016063614.2023.pdf43add30d4b4747a695ddb85fc20a415dMD56LICENSElicense.txtlicense.txttext/plain; charset=utf-85879https://repositorio.unal.edu.co/bitstream/unal/85642/5/license.txteb34b1cf90b7e1103fc9dfd26be24b4aMD55THUMBNAIL1016063614.2023.pdf.jpg1016063614.2023.pdf.jpgGenerated 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