期刊
PHYTOCHEMISTRY
卷 72, 期 11-12, 页码 1424-1430出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.phytochem.2011.04.007
关键词
Neolignans; Licarin A; Structure-activity relationship; Schistosomicidal activity; Trypanocidal activity
资金
- Fundacao de Amparo a Pesquisa do Estado de Sao Paulo (FAPESP) [06/06267-5, 1998/14956-7, 2009/15207-4, 2009/05049-2]
- Coordenadoria de Aperfeicoamento de Pessoal do Ensino Superior (CAPES)
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
(+/-)-Licarin A (1) was obtained by oxidative coupling, and its enantiomers, (-)-licarin A (2) and (+)-licarin A (3), were resolved by chiral HPLC. Schistosomicidal and trypanocidal activities of these compounds were evaluated in vitro against Schistosoma mansoni adult worms and trypomastigote forms of Trypanosoma cruzi. The racemic mixture (1) displayed significant schistosomicidal activity with an LC50 value of 53.57 mu M and moderate trypanocidal activity with an IC50 value of 127.17 mu M. On the other hand, the (-)-enantiomer (2), displaying a LC50 value of 91.71 mu M, was more active against S. mansoni than the (+)-enantiomer (3), which did not show activity. For the trypanocidal assay, enantiomer 2 showed more significant activity (IC50 of 23.46 mu M) than enantiomer 3, which showed an IC50 value of 87.73 mu M. Therefore, these results suggest that (+/-)-licarin A (1) and (-)-licarin A (2) are promising compounds that could be used for the development of schistosomicidal and trypanocidal agents. (C) 2011 Elsevier Ltd. All rights reserved.
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