Borges Carly H G, Cruz Michele G, Carneiro Luiza J, da Silva Jonas J M, Bastos Jairo K, Tavares Denise C, de Oliveira Pollyanna F, Rodrigues Vanderlei, Veneziani Rodrigo C S, Parreira Renato L T, Caramori Giovanni F, Nagurniak Gláucio R, Magalhães Lizandra G, Ambrósio Sérgio R
Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, 14404-600,, SP, Brazil.
School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, São Paulo, 14040-020,, SP, Brazil.
Chem Biodivers. 2016 Oct;13(10):1348-1356. doi: 10.1002/cbdv.201600065.
In this article, the in vitro schistosomicidal effects of three Brazilian Copaifera oleoresins (C. duckei, C. langsdorffii, and C. reticulata) are reported. From these botanical sources, the oleoresin of C. duckei (OCd) demonstrated to be the most promising, displaying LC values of 75.8, 50.6, and 47.2 μg/ml at 24, 48, and 72 h of incubation, respectively, against adult worms of Schistosoma mansoni, with a selectivity index of 10.26. Therefore, the major compounds from OCd were isolated, and the diterpene, (-)-polyalthic acid (PA), showed to be active (LC values of 41.7, 36.2, and 33.4 μg/ml, respectively, at 24, 48, and 72 h of incubation). Moreover, OCd and PA affected the production and development of eggs, and OCd modified the functionality of the tegument of S. mansoni. Possible synergistic and/or additive effects of this balsam were also verified when a mixture of the two of its main compounds (PA and ent-labd-8(17)-en-15,18-dioic acid) in the specific proportion of 3:1 (w/w) was tested. The obtained results indicate that PA should be considered for further investigations against S. mansoni, such as, synergistic (combination with praziquantel (PZQ)) and in vivo studies. It also shows that diterpenes are an important class of natural compounds for the investigation of agents capable of fighting the parasite responsible for human schistosomiasis.
本文报道了三种巴西苦配巴油树脂(杜克苦配巴、朗氏苦配巴和网脉苦配巴)的体外杀血吸虫作用。从这些植物来源中,杜克苦配巴油树脂(OCd)显示出最有前景的效果,在24、48和72小时的孵育后,对曼氏血吸虫成虫的LC值分别为75.8、50.6和47.2μg/ml,选择性指数为10.26。因此,从OCd中分离出主要化合物,二萜类化合物(-)-聚阿尔泰酸(PA)显示具有活性(在24、48和72小时孵育时的LC值分别为41.7、36.2和33.4μg/ml)。此外,OCd和PA影响虫卵的产生和发育,并且OCd改变了曼氏血吸虫体表的功能。当测试其两种主要化合物(PA和对映-半日花-8(17)-烯-15,18-二酸)按3:1(w/w)的特定比例混合时,也证实了这种香脂可能存在的协同和/或相加作用。所得结果表明,PA应考虑进一步针对曼氏血吸虫进行研究,例如协同作用(与吡喹酮(PZQ)联合)和体内研究。研究还表明,二萜类化合物是一类重要的天然化合物,可用于研究能够对抗引起人类血吸虫病寄生虫的药物。