Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells

Detalhes bibliográficos
Autor(a) principal: Ramalhete, Cátia
Data de Publicação: 2009
Outros Autores: Duarte, N, Capucha, V, Molnár, J, Mulhovo, S, Rosário, V, Ferreira, MJU
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10884/480
Resumo: The overexpression of P- glycoprotein (P-gp) is one of the mechanisms of multidrug resistance (MDR), responsible for the failure of cancer treatment. One strategy to restore the effectiveness of the anti-cancer drugs is to co-administer compounds that are not toxic themselves, but inhibit these efflux pumps. These compounds have been called MDR inhibitors, MDR modulators, MDR reversal agents or chemosensitizers (Fig.1). In recent years, several compounds have been reported as MDR modulators, obtained either from natural origin or by synthesis. However, in spite of the great number of MDR inhibitors known, no effective modulator without side effects is still available for the clinical practice.1 The aim of this study was to search for new multidrug reversal agents from Momordica balsamina L. (Fig.2). In this way, three new cucurbitane-type triterpenoids (1-3), a known compound (4) and five new acylated derivatives (5-9) prepared through acylation reactions of compound 4, have been evaluated for their potential ability as MDR modulators (Fig.3). Furthermore, the antiproliferative effects of the anticancer drug doxorubicin and the most effective modulators, in combination, was also studied.
id RCAP_3b80ed94960e948636b5b9ffbd718b56
oai_identifier_str oai:repositorio-cientifico.uatlantica.pt:10884/480
network_acronym_str RCAP
network_name_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository_id_str 7160
spelling Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cellsTriterpenesCancer cellsThe overexpression of P- glycoprotein (P-gp) is one of the mechanisms of multidrug resistance (MDR), responsible for the failure of cancer treatment. One strategy to restore the effectiveness of the anti-cancer drugs is to co-administer compounds that are not toxic themselves, but inhibit these efflux pumps. These compounds have been called MDR inhibitors, MDR modulators, MDR reversal agents or chemosensitizers (Fig.1). In recent years, several compounds have been reported as MDR modulators, obtained either from natural origin or by synthesis. However, in spite of the great number of MDR inhibitors known, no effective modulator without side effects is still available for the clinical practice.1 The aim of this study was to search for new multidrug reversal agents from Momordica balsamina L. (Fig.2). In this way, three new cucurbitane-type triterpenoids (1-3), a known compound (4) and five new acylated derivatives (5-9) prepared through acylation reactions of compound 4, have been evaluated for their potential ability as MDR modulators (Fig.3). Furthermore, the antiproliferative effects of the anticancer drug doxorubicin and the most effective modulators, in combination, was also studied.2012-03-06T13:27:15Z2009-01-01T00:00:00Z2009conference objectinfo:eu-repo/semantics/publishedVersionapplication/pdfhttp://hdl.handle.net/10884/480engRamalhete, CátiaDuarte, NCapucha, VMolnár, JMulhovo, SRosário, VFerreira, MJUinfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2024-10-31T15:59:26Zoai:repositorio-cientifico.uatlantica.pt:10884/480Portal AgregadorONGhttps://www.rcaap.pt/oai/openairemluisa.alvim@gmail.comopendoar:71602024-10-31T15:59:26Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãofalse
dc.title.none.fl_str_mv Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
title Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
spellingShingle Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
Ramalhete, Cátia
Triterpenes
Cancer cells
title_short Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
title_full Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
title_fullStr Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
title_full_unstemmed Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
title_sort Inhibition of P-glycoprotein activity by cucurbitane-type triterpenes and their interaction with doxorubicin on resistant cancer cells
author Ramalhete, Cátia
author_facet Ramalhete, Cátia
Duarte, N
Capucha, V
Molnár, J
Mulhovo, S
Rosário, V
Ferreira, MJU
author_role author
author2 Duarte, N
Capucha, V
Molnár, J
Mulhovo, S
Rosário, V
Ferreira, MJU
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv Ramalhete, Cátia
Duarte, N
Capucha, V
Molnár, J
Mulhovo, S
Rosário, V
Ferreira, MJU
dc.subject.por.fl_str_mv Triterpenes
Cancer cells
topic Triterpenes
Cancer cells
description The overexpression of P- glycoprotein (P-gp) is one of the mechanisms of multidrug resistance (MDR), responsible for the failure of cancer treatment. One strategy to restore the effectiveness of the anti-cancer drugs is to co-administer compounds that are not toxic themselves, but inhibit these efflux pumps. These compounds have been called MDR inhibitors, MDR modulators, MDR reversal agents or chemosensitizers (Fig.1). In recent years, several compounds have been reported as MDR modulators, obtained either from natural origin or by synthesis. However, in spite of the great number of MDR inhibitors known, no effective modulator without side effects is still available for the clinical practice.1 The aim of this study was to search for new multidrug reversal agents from Momordica balsamina L. (Fig.2). In this way, three new cucurbitane-type triterpenoids (1-3), a known compound (4) and five new acylated derivatives (5-9) prepared through acylation reactions of compound 4, have been evaluated for their potential ability as MDR modulators (Fig.3). Furthermore, the antiproliferative effects of the anticancer drug doxorubicin and the most effective modulators, in combination, was also studied.
publishDate 2009
dc.date.none.fl_str_mv 2009-01-01T00:00:00Z
2009
2012-03-06T13:27:15Z
dc.type.driver.fl_str_mv conference object
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://hdl.handle.net/10884/480
url http://hdl.handle.net/10884/480
dc.language.iso.fl_str_mv eng
language eng
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron:RCAAP
instname_str Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
instacron_str RCAAP
institution RCAAP
reponame_str Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
collection Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
repository.name.fl_str_mv Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação
repository.mail.fl_str_mv mluisa.alvim@gmail.com
_version_ 1817548668118499328