N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies

Autores
Lenis Rojas, Oscar A.; Cordeiro, Sandra; Horta Meireles, Marta; Fernández, Jhonathan Angel Araujo; Vila, Sabela Fernández; Rubiolo, Juan Andrés; Cabezas Sainz, Pablo; Sanchez, Laura; Fernandes, Alexandra R.; Royo, Beatriz
Año de publicación
2021
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.
Fil: Lenis Rojas, Oscar A.. Instituto de Tecnologia Química e Biológica António Xavier; Portugal
Fil: Cordeiro, Sandra. Universidade Nova de Lisboa; Portugal
Fil: Horta Meireles, Marta. Instituto de Tecnologia Química e Biológica António Xavier; Portugal
Fil: Fernández, Jhonathan Angel Araujo. Universidade Estadual de Campinas; Brasil. Universidad de Santiago de Compostela; España
Fil: Vila, Sabela Fernández. Universidad de Santiago de Compostela; España
Fil: Rubiolo, Juan Andrés. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Laboratorio de Biotecnología Acuática; Argentina. Universidad de Santiago de Compostela; España. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
Fil: Cabezas Sainz, Pablo. Universidad de Santiago de Compostela; España
Fil: Sanchez, Laura. Universidad de Santiago de Compostela; España
Fil: Fernandes, Alexandra R.. Universidade Nova de Lisboa; Portugal
Fil: Royo, Beatriz. Universidade Nova de Lisboa; Portugal
Materia
ANTICANCER ACTIVITY
IRON(II)–NHC COMPLEXES
N-HETEROCYCLIC CARBENE
ZEBRAFISH
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/153537
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/153537
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studiesLenis Rojas, Oscar A.Cordeiro, SandraHorta Meireles, MartaFernández, Jhonathan Angel AraujoVila, Sabela FernándezRubiolo, Juan AndrésCabezas Sainz, PabloSanchez, LauraFernandes, Alexandra R.Royo, BeatrizANTICANCER ACTIVITYIRON(II)–NHC COMPLEXESN-HETEROCYCLIC CARBENEZEBRAFISHhttps://purl.org/becyt/ford/1.6https://purl.org/becyt/ford/1Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.Fil: Lenis Rojas, Oscar A.. Instituto de Tecnologia Química e Biológica António Xavier; PortugalFil: Cordeiro, Sandra. Universidade Nova de Lisboa; PortugalFil: Horta Meireles, Marta. Instituto de Tecnologia Química e Biológica António Xavier; PortugalFil: Fernández, Jhonathan Angel Araujo. Universidade Estadual de Campinas; Brasil. Universidad de Santiago de Compostela; EspañaFil: Vila, Sabela Fernández. Universidad de Santiago de Compostela; EspañaFil: Rubiolo, Juan Andrés. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Laboratorio de Biotecnología Acuática; Argentina. Universidad de Santiago de Compostela; España. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; ArgentinaFil: Cabezas Sainz, Pablo. Universidad de Santiago de Compostela; EspañaFil: Sanchez, Laura. Universidad de Santiago de Compostela; EspañaFil: Fernandes, Alexandra R.. Universidade Nova de Lisboa; PortugalFil: Royo, Beatriz. Universidade Nova de Lisboa; PortugalMultidisciplinary Digital Publishing Institute2021-09info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/153537Lenis Rojas, Oscar A.; Cordeiro, Sandra; Horta Meireles, Marta; Fernández, Jhonathan Angel Araujo; Vila, Sabela Fernández; et al.; N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies; Multidisciplinary Digital Publishing Institute; Molecules; 26; 18; 9-2021; 1-141420-3049CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules26185535info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:51:13Zoai:ri.conicet.gov.ar:11336/153537instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-03 09:51:13.905CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
title N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
spellingShingle N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
Lenis Rojas, Oscar A.
ANTICANCER ACTIVITY
IRON(II)–NHC COMPLEXES
N-HETEROCYCLIC CARBENE
ZEBRAFISH
title_short N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
title_full N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
title_fullStr N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
title_full_unstemmed N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
title_sort N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies
dc.creator.none.fl_str_mv Lenis Rojas, Oscar A.
Cordeiro, Sandra
Horta Meireles, Marta
Fernández, Jhonathan Angel Araujo
Vila, Sabela Fernández
Rubiolo, Juan Andrés
Cabezas Sainz, Pablo
Sanchez, Laura
Fernandes, Alexandra R.
Royo, Beatriz
author Lenis Rojas, Oscar A.
author_facet Lenis Rojas, Oscar A.
Cordeiro, Sandra
Horta Meireles, Marta
Fernández, Jhonathan Angel Araujo
Vila, Sabela Fernández
Rubiolo, Juan Andrés
Cabezas Sainz, Pablo
Sanchez, Laura
Fernandes, Alexandra R.
Royo, Beatriz
author_role author
author2 Cordeiro, Sandra
Horta Meireles, Marta
Fernández, Jhonathan Angel Araujo
Vila, Sabela Fernández
Rubiolo, Juan Andrés
Cabezas Sainz, Pablo
Sanchez, Laura
Fernandes, Alexandra R.
Royo, Beatriz
author2_role author
author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv ANTICANCER ACTIVITY
IRON(II)–NHC COMPLEXES
N-HETEROCYCLIC CARBENE
ZEBRAFISH
topic ANTICANCER ACTIVITY
IRON(II)–NHC COMPLEXES
N-HETEROCYCLIC CARBENE
ZEBRAFISH
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.
Fil: Lenis Rojas, Oscar A.. Instituto de Tecnologia Química e Biológica António Xavier; Portugal
Fil: Cordeiro, Sandra. Universidade Nova de Lisboa; Portugal
Fil: Horta Meireles, Marta. Instituto de Tecnologia Química e Biológica António Xavier; Portugal
Fil: Fernández, Jhonathan Angel Araujo. Universidade Estadual de Campinas; Brasil. Universidad de Santiago de Compostela; España
Fil: Vila, Sabela Fernández. Universidad de Santiago de Compostela; España
Fil: Rubiolo, Juan Andrés. Universidad Nacional de Rosario. Facultad de Ciencias Bioquímicas y Farmacéuticas. Laboratorio de Biotecnología Acuática; Argentina. Universidad de Santiago de Compostela; España. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Rosario; Argentina
Fil: Cabezas Sainz, Pablo. Universidad de Santiago de Compostela; España
Fil: Sanchez, Laura. Universidad de Santiago de Compostela; España
Fil: Fernandes, Alexandra R.. Universidade Nova de Lisboa; Portugal
Fil: Royo, Beatriz. Universidade Nova de Lisboa; Portugal
description Cisplatin and its derivatives are commonly used in chemotherapeutic treatments of cancer, even though they suffer from many toxic side effects. The problems that emerge from the use of these metal compounds led to the search for new complexes capable to overcome the toxic side effects. Here, we report the evaluation of the antiproliferative activity of Fe(II) cyclopentadienyl complexes bearing n-heterocyclic carbene ligands in tumour cells and their in vivo toxicological profile. The in vitro antiproliferative assays demonstrated that complex Fe1 displays the highest cytotoxic activity both in human colorectal carcinoma cells (HCT116) and ovarian carcinoma cells (A2780) with IC50 values in the low micromolar range. The antiproliferative effect of Fe1 was even higher than cisplatin. Interestingly, Fe1 showed low in vivo toxicity, and in vivo analyses of Fe1 and Fe2 compounds using colorectal HCT116 zebrafish xenograft showed that both reduce the proliferation of human HCT116 colorectal cancer cells in vivo.
publishDate 2021
dc.date.none.fl_str_mv 2021-09
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 http://hdl.handle.net/11336/153537
Lenis Rojas, Oscar A.; Cordeiro, Sandra; Horta Meireles, Marta; Fernández, Jhonathan Angel Araujo; Vila, Sabela Fernández; et al.; N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies; Multidisciplinary Digital Publishing Institute; Molecules; 26; 18; 9-2021; 1-14
1420-3049
CONICET Digital
CONICET
url http://hdl.handle.net/11336/153537
identifier_str_mv Lenis Rojas, Oscar A.; Cordeiro, Sandra; Horta Meireles, Marta; Fernández, Jhonathan Angel Araujo; Vila, Sabela Fernández; et al.; N-heterocyclic carbene iron complexes as anticancer agents: In vitro and in vivo biological studies; Multidisciplinary Digital Publishing Institute; Molecules; 26; 18; 9-2021; 1-14
1420-3049
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/
info:eu-repo/semantics/altIdentifier/doi/10.3390/molecules26185535
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by/2.5/ar/
dc.format.none.fl_str_mv application/pdf
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:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
_version_ 1842269081341788160
score 13.13397

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