Mehlhorn H, Kojima S, Rim H J, Ruenwongsa P, Andrews P, Thomas H, Bunnag B
Arzneimittelforschung. 1983;33(1):91-8.
The effect of praziquantel (Biltricide) on the ultrastructure of trematodes pathogenic to man in Asia was investigated in: Clonorchis sinensis, Opisthorchis viverrini, Schistosoma japonicum, Metagonimus yokogawai, and Paragonimus westermani. The different parasites were isolated from their respective experimental hosts and uniformly incubated for 5, 15, 30 or 60 min at 37 degrees C in medium TC 199 containing 0, 1, 10 or 100 micrograms praziquantel/ml. All parasites exposed to praziquantel were contracted and displayed tegumental alterations. 1. Clonorchis sinensis, Opisthorchis viverrini and Schistosoma japonicum reacted with severe tegumental vacuolisation within 5 min after exposure to 1 microgram praziquantel/ml. The extent of the damage induced increased with exposure time. 2. In vivo treated Opisthorchis viverrini worms had the same damages as in vitro treated ones. 3. Metagonimus yokogawai displayed the same degree of vacuolisation after exposure to all concentrations of praziquantel. Complete destruction of the tegumental surface was not achieved, however, possibly because of the presence of numerous tegumental hooks. 4. Paragonimus westermani was least sensitive to praziquantel. Only very few vacuoles were formed after incubation in 100 micrograms/ml for 60 min. It is assumed that the very dense texture of the thick tegument is responsible for the relative refractoriness to praziquantel in vitro. However, in vivo the parasite is successfully eliminated by praziquantel.
研究了吡喹酮(拜尔晶)对亚洲人体致病吸虫超微结构的影响,这些吸虫包括:华支睾吸虫、湄公河平腹吸虫、日本血吸虫、横川后殖吸虫和卫氏并殖吸虫。将不同的寄生虫从各自的实验宿主中分离出来,在含有0、1、10或100微克/毫升吡喹酮的TC 199培养基中于37℃均匀孵育5、15、30或60分钟。所有接触吡喹酮的寄生虫均出现收缩并表现出体表改变。1. 华支睾吸虫、湄公河平腹吸虫和日本血吸虫在接触1微克/毫升吡喹酮后5分钟内即出现严重的体表空泡化。损伤程度随暴露时间增加。2. 体内处理的湄公河平腹吸虫虫体与体外处理的虫体损伤相同。3. 横川后殖吸虫在接触所有浓度的吡喹酮后均表现出相同程度的空泡化。然而,体表表面并未完全破坏,可能是因为存在大量体表钩。4. 卫氏并殖吸虫对吡喹酮最不敏感。在100微克/毫升中孵育60分钟后仅形成极少的空泡。推测厚体表的非常致密的质地是其在体外对吡喹酮相对不敏感的原因。然而,在体内该寄生虫可被吡喹酮成功清除。