Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.
Chem Biodivers. 2012 Aug;9(8):1465-74. doi: 10.1002/cbdv.201100336.
The schistosomicidal effects of pimaradienoic acid (PA) and two derivatives, obtained by fungal transformation in the presence of Aspergillus ochraceus, were investigated. PA was the only compound with antischistosomal activity among the three diterpenes studied, with the ability to significantly reduce the viability of the parasites at concentrations ranging from 25 to 100 μM. PA also promoted morphological alterations of the tegument of Schistosoma mansoni, separated all the worm couples, and affected the production and development of eggs. Moreover, this compound was devoid of toxicity toward human fibroblasts. In a preliminary in vivo experiment, PA at a dose of 100 mg/kg significantly diminished the number of parasites in infected Balb/c mice. Taken together, these results show that PA may be potentially employed in the discovery of novel schistosomicidal agents, and that diterpenes are an important class of natural compounds for the investigation of agents capable of fighting the parasite responsible for human schistosomiasis.
我们研究了枞酸（PA）及其两种衍生物的杀血吸虫效果，这些衍生物是在赭曲霉存在的条件下通过真菌转化获得的。在研究的三种二萜中，只有 PA 具有抗血吸虫活性，其在 25 至 100 μM 的浓度范围内能够显著降低寄生虫的活力。PA 还可促进曼氏血吸虫表皮的形态改变，使所有的虫对分离，并影响卵的产生和发育。此外，该化合物对人成纤维细胞没有毒性。在初步的体内实验中，100mg/kg 的 PA 可显著减少感染 Balb/c 小鼠体内的寄生虫数量。综上所述，这些结果表明 PA 可能有潜力用于发现新型杀血吸虫药物，二萜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的寄生虫的药物。
