Advanced search
Start date
Betweenand
Related content
(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Schistosomicidal and trypanocidal structure-activity relationships for (+/-)-licarin A and its (-)- and (+)-enantiomers

Full text
Author(s):
Show less -
Pereira, A. C. [1] ; Magalhaes, L. G. [1] ; Goncalves, U. O. [1] ; Luz, P. P. [1] ; Moraes, A. C. G. [1] ; Rodrigues, V. [2] ; da Matta Guedes, P. M. [3] ; da Silva Filho, A. A. [1] ; Cunha, W. R. [1] ; Bastos, J. K. [4] ; Nanayakkara, N. P. D. [5] ; e Silva, M. L. A. [1]
Total Authors: 12
Affiliation:
[1] Univ Franca, Grp Pesquisas Prod Nat, Nucleo Ciencias Exatas & Tecnol, BR-14404600 Franca, SP - Brazil
[2] Univ Sao Paulo, Dept Bioquim & Imunol, Fac Med Ribeirao Preto, BR-14049900 Sao Paulo - Brazil
[3] Univ Fed Rio Grande do Norte, Dept Microbiol & Parasitol, Ctr Biociencias, BR-59078900 Natal, RN - Brazil
[4] Univ Sao Paulo, Dept Ciencias Farmaceut, Fac Ciencias Farmaceut Ribeirao Preto, BR-14040903 Ribeirao Preto, SP - Brazil
[5] Univ Mississippi, Natl Ctr Nat Prod Res, Sch Pharm, Thad Cochran Res Ctr, University, MS 38677 - USA
Total Affiliations: 5
Document type: Journal article
Source: Phytochemistry; v. 72, n. 11-12, p. 1424-1430, AUG 2011.
Web of Science Citations: 26
Abstract

(+/-)-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. (AU)

FAPESP's process: 09/05049-2 - Development of polymeric nanaparticles and biodegradable systems containing lignans and evaluation its Chagas disease and schistosomiasis activities in vitro and in vivo
Grantee:Márcio Luís Andrade e Silva
Support Opportunities: Regular Research Grants
FAPESP's process: 09/15207-4 - Evaluation of the effect of lignans and neolignans on Schistosoma mansoni: a proteomic study
Grantee:Lizandra Guidi Magalhães
Support Opportunities: Scholarships in Brazil - Post-Doctoral