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Doctoral Thesis
DOI
https://doi.org/10.11606/T.87.2012.tde-21092012-104513
Document
Author
Full name
Ludmila Nakamura Rapado
Institute/School/College
Knowledge Area
Date of Defense
Published
São Paulo, 2012
Supervisor
Committee
Nakano, Eliana (President)
Cardoso, André Gustavo Tempone
Mendonça, Ronaldo Zucatelli
Paes, João Tadeu Ribeiro
Tuan, Roseli
Title in Portuguese
Obtenção e avaliação da atividade de compostos isolados de Piper em modelos biológicos para o controle da esquistossomose mansônica.
Keywords in Portuguese
Biomphalaria
Compostos moluscicida
Esquistossomose mansoni
Esquistossomose mansoni (toxicidade)
Fracionamento biomonitorado
Prevenção de doenças
Abstract in Portuguese
A esquistossomose é incidente em países tropicais e subtropicais e o uso de moluscicidas é adequado para prevenir a infecção de pessoas. O objetivo deste estudo foi buscar compostos em Piper ativos em Biomphalaria glabrata e avaliar a atividade esquistossomicida e toxicidade do composto mais ativo. O fracionamento biomonitorado de Piper diospyrifolium resultou no isolamento da flavocavaína A e ácido 4-hidroxi-3-[3,7,11-trimetildodeca-2,6,10-trienil]benzoico. A busca de compostos também foi realizada em amidas e chalconas e dos oito compostos avaliados, quatro foram ativos, sendo a piplartina mais ativa. A piplartina não foi letal a miracídios e cercárias de Schistosoma mansoni e foi tóxica em Daphnia similis e Danio rerio, contudo ainda foi menos tóxica que a niclosamida. Neste estudo, os compostos moluscicidas foram obtidos pelo fracionamento biomonitorado de P. diospyrifolium e pela avaliação da atividade de amidas e chalconas. Ambas as metodologias foram adequadas e a análise de componente principal mostrou ser uma ferramenta viável para a busca de compostos.
Title in English
Obtention an evaluation of Piper compounds in biological models to schistosomiasis mansoni control.
Keywords in English
Bioassay-guided fractionation
Biomphalaria
Molluscicidal compounds
Prevention of diseases
Schistosomiasis mansoni
Schistosomiasis mansoni (toxicity)
Abstract in English
Schistosomiasis is a parasitic disease and the use of molluscicides has been considered an appropriate method to prevent human infection. The aim of this study was to search for compounds in Piper active in B. glabrata and evaluate schistosomicidal activity and toxicity of the most active compound. The P. diospyrifolium bioguided fractionation resulted in flavokavain A and 4-hydroxy-3-[3,7,trimetildodeca-11-2,6,10-trienil]benzoic acid isolation. The search for active compounds was carried out in amides and chalcones. Eight compounds were evaluated, four were active and piplartine was the most active. There was no mortality of miracidia and cercariae exposed to piplartine. It was classified as toxic to D. similis and D. rerio; nevertheless was less toxic than niclosamide. In this study, molluscicidal compounds were obtained from bioguided fractionation of P.diospyrifolium and by evaluating the activity of amides and chalcones. Both methods were suitable to obtain active compounds and principal component analysis also proved to be a viable tool for obtain compounds.
 
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Publishing Date
2012-10-17
 
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