Laboratório de Parasitologia, Instituto Butantan, São Paulo, Brazil.
Exp Parasitol. 2011 Feb;127(2):357-64. doi: 10.1016/j.exppara.2010.08.021. Epub 2010 Sep 9.
Schistosomiasis is one of the world's greatly neglected tropical diseases, and its control is largely dependent on a single drug, praziquantel. Here, we report the in vitro effect of piplartine, an amide isolated from Piper tuberculatum (Piperaceae), on Schistosoma mansoni adult worms. A piplartine concentration of 15.8 μM reduced the motor activity of worms and caused their death within 24h in a RPMI 1640 medium. Similarly, the highest sub-lethal concentration of piplartine (6.3 μM) caused a 75% reduction in egg production in spite of coupling. Additionally, piplartine induced morphological changes on the tegument, and a quantitative analysis carried out by confocal microscopy revealed an extensive tegumental destruction and damage in the tubercles. This damage was dose-dependent in the range of 15.8-630.2 μM. At doses higher than 157.6 μM, piplartine induced morphological changes in the oral and ventral sucker regions of the worms. It is the first time that the schistosomicidal activity has been reported for piplartine.
血吸虫病是世界上被极大忽视的热带病之一,其控制在很大程度上依赖于一种单一的药物——吡喹酮。在这里,我们报告了从胡椒属植物(胡椒科)分离得到的酰胺哌啶,即胡椒丁胺,对曼氏血吸虫成虫的体外作用。在 RPMI 1640 培养基中,胡椒丁胺浓度为 15.8μM 即可降低虫体的运动活性,并在 24 小时内导致其死亡。同样,胡椒丁胺的最高亚致死浓度(6.3μM)尽管与伴侣结合,也会导致产卵减少 75%。此外,胡椒丁胺诱导表皮发生形态变化,通过共聚焦显微镜进行的定量分析显示,表皮在结节处广泛受损。这种损伤在 15.8-630.2μM 范围内呈剂量依赖性。在高于 157.6μM 的剂量下,胡椒丁胺会诱导虫体口吸盘和腹吸盘区域的形态变化。这是首次报道胡椒丁胺具有杀血吸虫活性。