Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones

This article belongs to the Section Biologics and Biosimilars.

Detalles Bibliográficos
Autores: Mármol, Inés, Quero, Javier, Azcárate, Paula, Atrián-Blasco, Elena, Ramos, Carla, Santos, Joana, Gimeno, M. Concepción, Rodríguez-Yoldi, María Jesús, Cerrada, Elena
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2022
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/303530
Acceso en línea:http://hdl.handle.net/10261/303530
Access Level:acceso abierto
Palabra clave:Alkynyl
Thioredoxin reductase
N-heterocyclic carbene
Dihydrofolate reductase
Gold complexes
Anticancer
Hydroxyflavones
Antibacterial
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spelling Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavonesMármol, InésQuero, JavierAzcárate, PaulaAtrián-Blasco, ElenaRamos, CarlaSantos, JoanaGimeno, M. ConcepciónRodríguez-Yoldi, María JesúsCerrada, ElenaAlkynylThioredoxin reductaseN-heterocyclic carbeneDihydrofolate reductaseGold complexesAnticancerHydroxyflavonesAntibacterialThis article belongs to the Section Biologics and Biosimilars.In this paper we describe the synthesis of new N-heterocyclic carbene (NHC) gold(I) derivatives with flavone-derived ligands with a propargyl ether group. The compounds were screened for their antimicrobial and anticancer activities, showing greater activity against bacteria than against colon cancer cells (Caco-2). Complexes [Au(L2b)(IMe)] (1b) and [Au(L2b)(IPr)] (2b) were found to be active against both Gram-positive and Gram-negative strains. The mechanism of action of 1b was evaluated by measurement of thioredoxin reductase (TrxR) and dihydrofolate reductase (DHFR) activity, besides scanning electron microscopy (SEM). Inhibition of the enzyme thioredoxin reductase is not observed in either Escherichia Coli or Caco-2 cells; however, DHFR activity is compromised after incubation of E. coli cells with complex 1b. Moreover, loss of structural integrity and change in bacterial shape is observed in the images obtained from scanning electron microscopy (SEM) after treatment E. coli cells with complex 1b.This research was funded by the Agencia Estatal de Investigación (projects PID2019-104379RB-C21/AEI/10.13039/501100011033, RED2018-102471-T/MCIN/AEI/10.13039/501100011033 and SAF2016-75441-R), CIBERobn under Grant (CB06/03/1012) of the Instituto Carlos III, European Grant Interreg/SUDOE (Redvalue, SOE1/PI/E0123) and Aragon Regional Government (B16-R17 and E07_20R).Peer reviewedMultidisciplinary Digital Publishing InstituteMinisterio de Ciencia, Innovación y Universidades (España)Agencia Estatal de Investigación (España)European CommissionInstituto de Salud Carlos IIIGobierno de AragónMinisterio de Economía y Competitividad (España)Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]202320232022info:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_6501Publisher's versioninfo:eu-repo/semantics/publishedVersionapplication/pdfhttp://hdl.handle.net/10261/303530reponame:DIGITAL.CSIC. Repositorio Institucional del CSICinstname:Consejo Superior de Investigaciones Científicas (CSIC)Inglés#PLACEHOLDER_PARENT_METADATA_VALUE##PLACEHOLDER_PARENT_METADATA_VALUE##PLACEHOLDER_PARENT_METADATA_VALUE#info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2019-104379RB-C21RED2018-102471-TSAF2016-75441-RPharmaceuticshttps://doi.org/10.3390/pharmaceutics14102064Síinfo:eu-repo/semantics/openAccessoai:digital.csic.es:10261/3035302026-05-22T06:33:51Z
dc.title.none.fl_str_mv Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
title Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
spellingShingle Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
Mármol, Inés
Alkynyl
Thioredoxin reductase
N-heterocyclic carbene
Dihydrofolate reductase
Gold complexes
Anticancer
Hydroxyflavones
Antibacterial
title_short Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
title_full Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
title_fullStr Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
title_full_unstemmed Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
title_sort Biological activity of NHC-Gold-alkynyl complexes derived from 3-hydroxyflavones
dc.creator.none.fl_str_mv Mármol, Inés
Quero, Javier
Azcárate, Paula
Atrián-Blasco, Elena
Ramos, Carla
Santos, Joana
Gimeno, M. Concepción
Rodríguez-Yoldi, María Jesús
Cerrada, Elena
author Mármol, Inés
author_facet Mármol, Inés
Quero, Javier
Azcárate, Paula
Atrián-Blasco, Elena
Ramos, Carla
Santos, Joana
Gimeno, M. Concepción
Rodríguez-Yoldi, María Jesús
Cerrada, Elena
author_role author
author2 Quero, Javier
Azcárate, Paula
Atrián-Blasco, Elena
Ramos, Carla
Santos, Joana
Gimeno, M. Concepción
Rodríguez-Yoldi, María Jesús
Cerrada, Elena
author2_role author
author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Ministerio de Ciencia, Innovación y Universidades (España)
Agencia Estatal de Investigación (España)
European Commission
Instituto de Salud Carlos III
Gobierno de Aragón
Ministerio de Economía y Competitividad (España)
Consejo Superior de Investigaciones Científicas [https://ror.org/02gfc7t72]
dc.subject.none.fl_str_mv Alkynyl
Thioredoxin reductase
N-heterocyclic carbene
Dihydrofolate reductase
Gold complexes
Anticancer
Hydroxyflavones
Antibacterial
topic Alkynyl
Thioredoxin reductase
N-heterocyclic carbene
Dihydrofolate reductase
Gold complexes
Anticancer
Hydroxyflavones
Antibacterial
description This article belongs to the Section Biologics and Biosimilars.
publishDate 2022
dc.date.none.fl_str_mv 2022
2023
2023
dc.type.none.fl_str_mv info:eu-repo/semantics/article
http://purl.org/coar/resource_type/c_6501
Publisher's version
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/10261/303530
url http://hdl.handle.net/10261/303530
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv #PLACEHOLDER_PARENT_METADATA_VALUE#
#PLACEHOLDER_PARENT_METADATA_VALUE#
#PLACEHOLDER_PARENT_METADATA_VALUE#
info:eu-repo/grantAgreement/AEI/Plan Estatal de Investigación Científica y Técnica y de Innovación 2017-2020/PID2019-104379RB-C21
RED2018-102471-T
SAF2016-75441-R
Pharmaceutics
https://doi.org/10.3390/pharmaceutics14102064
Sí
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Multidisciplinary Digital Publishing Institute
publisher.none.fl_str_mv Multidisciplinary Digital Publishing Institute
dc.source.none.fl_str_mv reponame:DIGITAL.CSIC. Repositorio Institucional del CSIC
instname:Consejo Superior de Investigaciones Científicas (CSIC)
instname_str Consejo Superior de Investigaciones Científicas (CSIC)
reponame_str DIGITAL.CSIC. Repositorio Institucional del CSIC
collection DIGITAL.CSIC. Repositorio Institucional del CSIC
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15.812429

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