In vitro schistosomicidal activity of balsaminol F and karavilagenin C.
Autor(a) principal: | |
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Data de Publicação: | 2012 |
Outros Autores: | , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10884/1313 |
Resumo: | Five cucurbitane-type triterpenes (1-5), previously isolated from the African medicinal plant Momordica balsamina, along with five ester derivatives (6-10) of karavilagenin C (2), were evaluated for their potential schistosomicidal activity against Schistosoma mansoni adult worms. The natural compounds were isolated from the ethyl acetate-soluble fraction of the methanol extract of the aerial parts of M. balsamina. In a preliminary study, a significant schistosomicidal activity was observed for both the crude methanol extract and the ethyl acetate fraction. The compounds responsible for the activity were found to be balsaminol F (1) and karavilagenin C (2) with LC50 values of 14.7 ± 1.5 and 28.9 ± 1.8 µM, respectively, after 24 h of incubation (positive control praziquantel, LC₅₀ = 1.2 ± 0.1 µM). Both compounds (1, 2), at 10-50 µM, induced significant reductions in the motor activity of the worms and significantly decreased the egg production. Furthermore, they were able (at 10-100 µM) to separate the adult worm pairs into male and female after 24 h. Compounds 3-5, bearing a sugar moiety as a substituent, and the acylated derivatives of karavilagenin C (6-10) were inactive, suggesting that the presence of free hydroxyl groups in the tetracyclic skeleton might be important for the activity. A correlation between activity and the molecular volume/weight of compounds was also found. |
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In vitro schistosomicidal activity of balsaminol F and karavilagenin C.Five cucurbitane-type triterpenes (1-5), previously isolated from the African medicinal plant Momordica balsamina, along with five ester derivatives (6-10) of karavilagenin C (2), were evaluated for their potential schistosomicidal activity against Schistosoma mansoni adult worms. The natural compounds were isolated from the ethyl acetate-soluble fraction of the methanol extract of the aerial parts of M. balsamina. In a preliminary study, a significant schistosomicidal activity was observed for both the crude methanol extract and the ethyl acetate fraction. The compounds responsible for the activity were found to be balsaminol F (1) and karavilagenin C (2) with LC50 values of 14.7 ± 1.5 and 28.9 ± 1.8 µM, respectively, after 24 h of incubation (positive control praziquantel, LC₅₀ = 1.2 ± 0.1 µM). Both compounds (1, 2), at 10-50 µM, induced significant reductions in the motor activity of the worms and significantly decreased the egg production. Furthermore, they were able (at 10-100 µM) to separate the adult worm pairs into male and female after 24 h. Compounds 3-5, bearing a sugar moiety as a substituent, and the acylated derivatives of karavilagenin C (6-10) were inactive, suggesting that the presence of free hydroxyl groups in the tetracyclic skeleton might be important for the activity. A correlation between activity and the molecular volume/weight of compounds was also found.Planta Medica2018-08-28T10:21:28Z2012-12-01T00:00:00Z2012-12info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://hdl.handle.net/10884/1313engRamalhete, CátiaMagalhães, L. G.Rodrigues, V.Mulhovo, SilvaDa Silva Filho, A. A.Ferreira, Maria Joséinfo: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:RCAAP2024-01-04T11:08:01Zoai:repositorio-cientifico.uatlantica.pt:10884/1313Portal AgregadorONGhttps://www.rcaap.pt/oai/openaireopendoar:71602024-03-20T01:29:53.455908Repositório 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 |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
title |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
spellingShingle |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. Ramalhete, Cátia |
title_short |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
title_full |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
title_fullStr |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
title_full_unstemmed |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
title_sort |
In vitro schistosomicidal activity of balsaminol F and karavilagenin C. |
author |
Ramalhete, Cátia |
author_facet |
Ramalhete, Cátia Magalhães, L. G. Rodrigues, V. Mulhovo, Silva Da Silva Filho, A. A. Ferreira, Maria José |
author_role |
author |
author2 |
Magalhães, L. G. Rodrigues, V. Mulhovo, Silva Da Silva Filho, A. A. Ferreira, Maria José |
author2_role |
author author author author author |
dc.contributor.author.fl_str_mv |
Ramalhete, Cátia Magalhães, L. G. Rodrigues, V. Mulhovo, Silva Da Silva Filho, A. A. Ferreira, Maria José |
description |
Five cucurbitane-type triterpenes (1-5), previously isolated from the African medicinal plant Momordica balsamina, along with five ester derivatives (6-10) of karavilagenin C (2), were evaluated for their potential schistosomicidal activity against Schistosoma mansoni adult worms. The natural compounds were isolated from the ethyl acetate-soluble fraction of the methanol extract of the aerial parts of M. balsamina. In a preliminary study, a significant schistosomicidal activity was observed for both the crude methanol extract and the ethyl acetate fraction. The compounds responsible for the activity were found to be balsaminol F (1) and karavilagenin C (2) with LC50 values of 14.7 ± 1.5 and 28.9 ± 1.8 µM, respectively, after 24 h of incubation (positive control praziquantel, LC₅₀ = 1.2 ± 0.1 µM). Both compounds (1, 2), at 10-50 µM, induced significant reductions in the motor activity of the worms and significantly decreased the egg production. Furthermore, they were able (at 10-100 µM) to separate the adult worm pairs into male and female after 24 h. Compounds 3-5, bearing a sugar moiety as a substituent, and the acylated derivatives of karavilagenin C (6-10) were inactive, suggesting that the presence of free hydroxyl groups in the tetracyclic skeleton might be important for the activity. A correlation between activity and the molecular volume/weight of compounds was also found. |
publishDate |
2012 |
dc.date.none.fl_str_mv |
2012-12-01T00:00:00Z 2012-12 2018-08-28T10:21:28Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10884/1313 |
url |
http://hdl.handle.net/10884/1313 |
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eng |
language |
eng |
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info:eu-repo/semantics/openAccess |
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openAccess |
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application/pdf |
dc.publisher.none.fl_str_mv |
Planta Medica |
publisher.none.fl_str_mv |
Planta Medica |
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reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
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Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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RCAAP |
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RCAAP |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) - Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
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