New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant

Detalhes bibliográficos
Autor(a) principal: Ramalhete, Cátia
Data de Publicação: 2009
Outros Autores: Spengler, G, Serley, J, Duarte, N, Viveiros, M, Amaral, L, Molnár, J, Mulhovo, S, Ferreira, MJU
Idioma: eng
Título da fonte: Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)
Texto Completo: http://hdl.handle.net/10884/481
Resumo: All living cells contain genes encoding multidrug transporters and some of them play an important role in conferring drug resistance in mammalian cancer cells and in microbial pathogens such as Staphylococcus aureus, Enterococcus faecalis, Candida albicans, Plasmodium falciparum, and Leishmania donovani. The over-expression of P- glycoprotein (P-gp) is one of the principal mechanisms of multidrug resistance (MDR) found in eukaryotic and prokaryotic cells (Fig.1). The inhibition of P-gp as a possible way of reversing MDR has been extensively studied. A large number of plant-derived compounds and synthetic molecules have been shown to block MDR pump efflux activity. Nevertheless, their pharmacokinetic interaction with chemotherapy and side effects have limited their clinical development.1 In our search for biologically active compounds from Momordica balsamina L. (Fig.2), we have isolated and characterized three new cucurbitane-type triterpenes, named balsaminagenin A and B, and balsaminoside A (1-3) and a known cucurbitacin (4). The isolated compounds (Fig.3) were evaluated for their efflux modulating effects of Gram positive and negative bacteria by a real-time fluorimetric method that utilizes the fluorochrome ethidium bromide (EB), a universal substrate of bacterial efflux pumps. Furthermore, the evaluation of the compounds as P-gp modulators of resistant cancer cells was also carried out by flow cytometry, using rhodamine 123, and by real-time fluorometry method, the latter method assessing accumulation of EB on a real-time basis.
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spelling New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plantAfrican medicinal plantCancerGram positive bacteriaAll living cells contain genes encoding multidrug transporters and some of them play an important role in conferring drug resistance in mammalian cancer cells and in microbial pathogens such as Staphylococcus aureus, Enterococcus faecalis, Candida albicans, Plasmodium falciparum, and Leishmania donovani. The over-expression of P- glycoprotein (P-gp) is one of the principal mechanisms of multidrug resistance (MDR) found in eukaryotic and prokaryotic cells (Fig.1). The inhibition of P-gp as a possible way of reversing MDR has been extensively studied. A large number of plant-derived compounds and synthetic molecules have been shown to block MDR pump efflux activity. Nevertheless, their pharmacokinetic interaction with chemotherapy and side effects have limited their clinical development.1 In our search for biologically active compounds from Momordica balsamina L. (Fig.2), we have isolated and characterized three new cucurbitane-type triterpenes, named balsaminagenin A and B, and balsaminoside A (1-3) and a known cucurbitacin (4). The isolated compounds (Fig.3) were evaluated for their efflux modulating effects of Gram positive and negative bacteria by a real-time fluorimetric method that utilizes the fluorochrome ethidium bromide (EB), a universal substrate of bacterial efflux pumps. Furthermore, the evaluation of the compounds as P-gp modulators of resistant cancer cells was also carried out by flow cytometry, using rhodamine 123, and by real-time fluorometry method, the latter method assessing accumulation of EB on a real-time basis.2012-03-06T13:35:50Z2009-01-01T00:00:00Z2009conference objectinfo:eu-repo/semantics/publishedVersionapplication/pdfhttp://hdl.handle.net/10884/481engRamalhete, CátiaSpengler, GSerley, JDuarte, NViveiros, MAmaral, LMolnár, JMulhovo, SFerreira, 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:10884/481Portal 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 New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
title New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
spellingShingle New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
Ramalhete, Cátia
African medicinal plant
Cancer
Gram positive bacteria
title_short New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
title_full New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
title_fullStr New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
title_full_unstemmed New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
title_sort New efflux pumps inhibitors for Gram positive bacteria strains and cancer cells from an African medicinal plant
author Ramalhete, Cátia
author_facet Ramalhete, Cátia
Spengler, G
Serley, J
Duarte, N
Viveiros, M
Amaral, L
Molnár, J
Mulhovo, S
Ferreira, MJU
author_role author
author2 Spengler, G
Serley, J
Duarte, N
Viveiros, M
Amaral, L
Molnár, J
Mulhovo, S
Ferreira, MJU
author2_role author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Ramalhete, Cátia
Spengler, G
Serley, J
Duarte, N
Viveiros, M
Amaral, L
Molnár, J
Mulhovo, S
Ferreira, MJU
dc.subject.por.fl_str_mv African medicinal plant
Cancer
Gram positive bacteria
topic African medicinal plant
Cancer
Gram positive bacteria
description All living cells contain genes encoding multidrug transporters and some of them play an important role in conferring drug resistance in mammalian cancer cells and in microbial pathogens such as Staphylococcus aureus, Enterococcus faecalis, Candida albicans, Plasmodium falciparum, and Leishmania donovani. The over-expression of P- glycoprotein (P-gp) is one of the principal mechanisms of multidrug resistance (MDR) found in eukaryotic and prokaryotic cells (Fig.1). The inhibition of P-gp as a possible way of reversing MDR has been extensively studied. A large number of plant-derived compounds and synthetic molecules have been shown to block MDR pump efflux activity. Nevertheless, their pharmacokinetic interaction with chemotherapy and side effects have limited their clinical development.1 In our search for biologically active compounds from Momordica balsamina L. (Fig.2), we have isolated and characterized three new cucurbitane-type triterpenes, named balsaminagenin A and B, and balsaminoside A (1-3) and a known cucurbitacin (4). The isolated compounds (Fig.3) were evaluated for their efflux modulating effects of Gram positive and negative bacteria by a real-time fluorimetric method that utilizes the fluorochrome ethidium bromide (EB), a universal substrate of bacterial efflux pumps. Furthermore, the evaluation of the compounds as P-gp modulators of resistant cancer cells was also carried out by flow cytometry, using rhodamine 123, and by real-time fluorometry method, the latter method assessing accumulation of EB on a real-time basis.
publishDate 2009
dc.date.none.fl_str_mv 2009-01-01T00:00:00Z
2009
2012-03-06T13:35:50Z
dc.type.driver.fl_str_mv conference object
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dc.identifier.uri.fl_str_mv http://hdl.handle.net/10884/481
url http://hdl.handle.net/10884/481
dc.language.iso.fl_str_mv eng
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dc.format.none.fl_str_mv application/pdf
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