Grupo de Pesquisas em Produtos Naturais, Núcleo de Ciências Exatas e Tecnológicas, Universidade de Franca, Avenida Dr. Armando Salles de Oliveira 2001, 14404-600 Franca, SP, Brazil.
Phytochemistry. 2011 Aug;72(11-12):1424-30. doi: 10.1016/j.phytochem.2011.04.007. Epub 2011 May 11.
(±)-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 μM and moderate trypanocidal activity with an IC₅₀ value of 127.17 μM. On the other hand, the (-)-enantiomer (2), displaying a LC₅₀ value of 91.71 μM, 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 μM) than enantiomer 3, which showed an IC₅₀ value of 87.73 μM. 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.
(±)-Licarin A（1）通过氧化偶联得到，其对映异构体（-）-licarin A（2）和（+）-licarin A（3）通过手性 HPLC 拆分。这些化合物对曼氏血吸虫成虫和克氏锥虫的动基体形式的杀血吸虫和杀锥虫活性在体外进行了评估。外消旋混合物（1）表现出显著的杀血吸虫活性，LC₅₀值为 53.57 μM，对锥虫具有中等的杀活性，IC₅₀值为 127.17 μM。另一方面，（-）-对映异构体（2）显示出比（+）-对映异构体（3）更高的抗曼氏血吸虫活性，其 LC₅₀值为 91.71 μM，而（+）-对映异构体（3）则没有活性。对于杀锥虫试验，对映异构体 2 显示出比对映异构体 3 更高的活性（IC₅₀为 23.46 μM），而对映异构体 3 的 IC₅₀值为 87.73 μM。因此，这些结果表明（±）-licarin A（1）和（-）-licarin A（2）是有前途的化合物，可用于开发杀血吸虫和杀锥虫剂。
