Flavonoids As DNA Topoisomerase I Poisons

The therapeutic anticancer potential of flavonoids shown by recent research needs a greater understanding of these compounds. They are antioxidants and antimutagenic agents that can inhibit tumor promotion and transformation and can modify the activity of a large number of mammalian enzyme systems,...

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Detalles Bibliográficos
Autores: López Lázaro, Miguel, Martín Cordero, Carmen, Toro, M. V., Ayuso, María Jesús
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2002
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/131994
Acceso en línea:https://hdl.handle.net/11441/131994
https://doi.org/10.1080/14756360290011744
Access Level:acceso abierto
Palabra clave:Topoisomerase poisons
SRB assay
Flavonols
Isoflavones
Myricetin
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spelling Flavonoids As DNA Topoisomerase I PoisonsLópez Lázaro, MiguelMartín Cordero, CarmenToro, M. V.Ayuso, María JesúsTopoisomerase poisonsSRB assayFlavonolsIsoflavonesMyricetinThe therapeutic anticancer potential of flavonoids shown by recent research needs a greater understanding of these compounds. They are antioxidants and antimutagenic agents that can inhibit tumor promotion and transformation and can modify the activity of a large number of mammalian enzyme systems, such as human DNAtopoisomerases. Poisons of topoisomerases generate toxic DNA damage by stabilization of the covalent DNA-topoisomerase cleavage complex and some of them have therapeutic efficacy in human cancer. The present investigation has assayed ten flavonoids, isolated in our laboratory, as topoisomerase I poisons obtaining myricetin and myricetin-3-galactoside as two new topoiosomerase I poisons. These two flavonoids, and the plant extract from which they were isolated, were assayed for cytotoxic activity against three human cancer cell lines using the SRB assay. Taking into account our previous research, structural requisites implicated in the topoisomerase poisoning are discussed.Ministerio de Ciencia y Tecnología de España. SAF 2000-0167Taylor & Francis Open AccessFarmacologíaMinisterio de Ciencia y Tecnología (MCYT). España2002info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/11441/131994https://doi.org/10.1080/14756360290011744reponame:idUS. Depósito de Investigación de la Universidad de Sevillainstname:Universidad de Sevilla (US)InglésJournal of Enzyme Inhibition and Medicinal Chemistry, 17 (1), 25-29.SAF 2000-0167https://doi.org/10.1080/14756360290011744info:eu-repo/semantics/openAccessoai:idus.us.es:11441/1319942026-06-17T12:51:07Z
dc.title.none.fl_str_mv Flavonoids As DNA Topoisomerase I Poisons
title Flavonoids As DNA Topoisomerase I Poisons
spellingShingle Flavonoids As DNA Topoisomerase I Poisons
López Lázaro, Miguel
Topoisomerase poisons
SRB assay
Flavonols
Isoflavones
Myricetin
title_short Flavonoids As DNA Topoisomerase I Poisons
title_full Flavonoids As DNA Topoisomerase I Poisons
title_fullStr Flavonoids As DNA Topoisomerase I Poisons
title_full_unstemmed Flavonoids As DNA Topoisomerase I Poisons
title_sort Flavonoids As DNA Topoisomerase I Poisons
dc.creator.none.fl_str_mv López Lázaro, Miguel
Martín Cordero, Carmen
Toro, M. V.
Ayuso, María Jesús
author López Lázaro, Miguel
author_facet López Lázaro, Miguel
Martín Cordero, Carmen
Toro, M. V.
Ayuso, María Jesús
author_role author
author2 Martín Cordero, Carmen
Toro, M. V.
Ayuso, María Jesús
author2_role author
author
author
dc.contributor.none.fl_str_mv Farmacología
Ministerio de Ciencia y Tecnología (MCYT). España
dc.subject.none.fl_str_mv Topoisomerase poisons
SRB assay
Flavonols
Isoflavones
Myricetin
topic Topoisomerase poisons
SRB assay
Flavonols
Isoflavones
Myricetin
description The therapeutic anticancer potential of flavonoids shown by recent research needs a greater understanding of these compounds. They are antioxidants and antimutagenic agents that can inhibit tumor promotion and transformation and can modify the activity of a large number of mammalian enzyme systems, such as human DNAtopoisomerases. Poisons of topoisomerases generate toxic DNA damage by stabilization of the covalent DNA-topoisomerase cleavage complex and some of them have therapeutic efficacy in human cancer. The present investigation has assayed ten flavonoids, isolated in our laboratory, as topoisomerase I poisons obtaining myricetin and myricetin-3-galactoside as two new topoiosomerase I poisons. These two flavonoids, and the plant extract from which they were isolated, were assayed for cytotoxic activity against three human cancer cell lines using the SRB assay. Taking into account our previous research, structural requisites implicated in the topoisomerase poisoning are discussed.
publishDate 2002
dc.date.none.fl_str_mv 2002
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/11441/131994
https://doi.org/10.1080/14756360290011744
url https://hdl.handle.net/11441/131994
https://doi.org/10.1080/14756360290011744
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Journal of Enzyme Inhibition and Medicinal Chemistry, 17 (1), 25-29.
SAF 2000-0167
https://doi.org/10.1080/14756360290011744
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Taylor & Francis Open Access
publisher.none.fl_str_mv Taylor & Francis Open Access
dc.source.none.fl_str_mv reponame:idUS. Depósito de Investigación de la Universidad de Sevilla
instname:Universidad de Sevilla (US)
instname_str Universidad de Sevilla (US)
reponame_str idUS. Depósito de Investigación de la Universidad de Sevilla
collection idUS. Depósito de Investigación de la Universidad de Sevilla
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,301603

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