Artículos de revistas
Schistosomicidal and trypanocidal structure-activity relationships for (+/-)-licarin A and its (-)- and (+)-enantiomers
Fecha
2011Registro en:
PHYTOCHEMISTRY, v.72, n.11/Dez, p.1424-1430, 2011
0031-9422
10.1016/j.phytochem.2011.04.007
Autor
PEREIRA, A. C.
MAGALHAES, L. G.
GONCALVES, U. O.
LUZ, P. P.
MORAES, A. C. G.
RODRIGUES, V.
GUEDES, P. M. da Matta
SILVA FILHO, A. A. da
CUNHA, W. R.
BASTOS, J. K.
NANAYAKKARA, N. P. D.
SILVA, M. L. A. e
Institución
Resumen
(+/-)-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 LC(50) value of 53.57 mu M and moderate trypanocidal activity with an IC(50) value of 127.17 mu M. On the other hand, the (-)-enantiomer (2), displaying a LC(50) 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 (IC(50) of 23.46 mu M) than enantiomer 3, which showed an IC(50) 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.