Document Detail


Antitrypanosomal activity of a diterpene and lignans isolated from Aristolochia cymbifera.
MedLine Citation:
PMID:  20301059     Owner:  NLM     Status:  In-Process    
Abstract/OtherAbstract:
Bioguided fractionation of extract from the leaves of Aristolochia cymbifera led to the isolation of the furofuran lignans fargesin, epieudesmin, and sesamin; the dibenzylbutyrolactone lignans hinokinin and kusunokinin; and an ENT-labdane diterpene named copalic acid. Our data demonstrated that copalic acid and kusunokinin were the most active compounds against trypomastigotes of Trypanosoma cruzi. Additionally, copalic acid demonstrated the highest parasite selectivity as a result of low toxicity to mammalian cells, despite a considerable hemolytic activity at higher concentrations. Among the isolated compounds, kusunokinin could be considered the most promising candidate, as it displayed significant activity against intracellular amastigotes (IC(50) = 17 µM) and trypomastigotes (IC(50) = 51 µM) without hemolytic activity. Fargesin, hinokinin, epieudesmin, and sesamin were also effective against trypomastigotes, but these compounds were highly toxic to mammalian cells and no parasite selectivity could be identified. The need for novel drugs for American trypanosomiasis is evident, and these secondary metabolites from A. cymbifera represent a useful tool for drug design.
Authors:
Patrícia Sartorelli; Camila Salomone Carvalho; Juliana Quero Reimão; Harri Lorenzi; André Gustavo Tempone
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-03-18
Journal Detail:
Title:  Planta medica     Volume:  76     ISSN:  1439-0221     ISO Abbreviation:  Planta Med.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-09-13     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0066751     Medline TA:  Planta Med     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  1454-6     Citation Subset:  IM    
Copyright Information:
© Georg Thieme Verlag KG Stuttgart-New York.
Affiliation:
Departamento de Ciências Exatas e da Terra, Universidade Federal de São Paulo, Diadema/São Paulo, Brazil. psartorelli@unifesp.br
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