Fairweather I, Anderson H R, Threadgold L T
Exp Parasitol. 1986 Dec;62(3):336-48. doi: 10.1016/0014-4894(86)90040-8.
The effect of the deacetylated (amine) metabolite of diamphenethide (10 mugm/ml) on the tegument of Fasciola hepatica over a 24 hr period in vitro has been determined by means of transmission electron microscopy. In the tegumental syncytium, there is an initial accumulation of T2 secretory bodies at the apical surface (after 6 hr), together with increased exocytosis of secretory bodies and blebbing of the surface membrane. After 9 hr, the two surfaces of the fluke show different tegumental responses to drug treatment with a marked swelling of the basal infolds in the dorsal tegument, while the ventral tegument remains normal. By 18 hr, the swelling in the dorsal tegument is very severe, the entire basal region becoming edematous. In some areas, the tegument becomes detached to expose the basal lamina. The ventral tegument retains a fairly normal morphology, although there is a slight swelling of the basal infolds. The edema spreads internally to the cell bodies, beginning after 9 hr on the dorsal side of the fluke and 18 hr on the ventral side. By 18 hr, the flooding on the dorsal side is very severe and the cells attenuated, retaining few contacts with the surrounding parenchyma. From 9 hr onwards, there are progressive changes in cell structure, including a decrease in amount of granular endoplasmic reticulum and extent of its ribosomal covering, a decrease in numbers of secretory bodies, a swelling of the trans-most Golgi cisternae and disruption of the release of secretory bodies, and a swelling and disorganization of the mitochondria. The results are discussed in relation to the postulated activity of the deacetylated (amine) metabolite of diamphenethide as a Na+ ionophore.
通过透射电子显微镜观察，已确定双胺苯噻酯的脱乙酰化（胺）代谢产物（10微克/毫升）在体外24小时内对肝片吸虫皮层的影响。在皮层合胞体中，T2分泌小体最初在顶端表面积累（6小时后），同时分泌小体的胞吐作用增加，表面膜出现泡状突起。9小时后，吸虫的两个表面对药物处理表现出不同的皮层反应，背侧皮层的基底褶皱明显肿胀，而腹侧皮层保持正常。到18小时时，背侧皮层的肿胀非常严重，整个基底区域变得水肿。在某些区域，皮层脱落，暴露出基膜。腹侧皮层保持相当正常的形态，尽管基底褶皱有轻微肿胀。水肿向内扩散到细胞体，在吸虫背侧9小时后开始，腹侧18小时后开始。到18小时时，背侧的水肿非常严重，细胞萎缩，与周围实质的接触很少。从9小时起，细胞结构发生渐进性变化，包括颗粒内质网数量及其核糖体覆盖范围减少、分泌小体数量减少、最外侧高尔基体池肿胀以及分泌小体释放中断，以及线粒体肿胀和紊乱。结合双胺苯噻酯的脱乙酰化（胺）代谢产物作为Na+离子载体的假定活性对结果进行了讨论。
