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Anthelmintic efficacy of natural saponins against Gyrodactylus kobayashii in goldfish ( Carassius auratus ) and their 3D-QSAR analysis
Parasitology Research ( IF 1.8 ) Pub Date : 2021-01-09 , DOI: 10.1007/s00436-020-07043-1
Shun Zhou 1, 2, 3 , Jing Dong 1, 3 , Yongtao Liu 1, 3 , Qiuhong Yang 1, 3 , Ning Xu 1, 3 , Yibin Yang 1, 3 , Xiaohui Ai 1, 3
Affiliation  

Gyrodactylus spp. are common monogenean ectoparasites that may lead to significant fish mortality. To find effective anthelmintic agents with lower toxicity, a series of natural saponins were obtained and evaluated for their anthelmintic activity against Gyrodactylus kobayashii and acute toxicity to goldfish (Carassius auratus). Among all tested compounds, six compounds (1, 2, 3, 8, 10, and 13) shown higher anthelmintic activity and safety than widely used formaldehyde-based parasiticides, especially compound 1 having 100% anthelmintic efficacy against G. kobayashii at 0.3 mg/L and a therapeutic index of 16.6. Also, the three-dimensional quantitative structure-activity relationship (3D-QSAR) studies of these saponins have been performed to explore the structural features reasonable for the anthelmintic activity against G. kobayashii. These models demonstrated that the hydroxyl group at C-17 position and the sugar moieties at C-3 position, especially the hydroxyl groups of the sugar moieties, were critical to the anthelmintic activity. The QSAR studies could provide useful information for further rational design and optimization of novel saponins for the control of gyrodactylosis.



中文翻译:

天然皂甙对小金刚鱼(Gassirodactylus kobayashii)在金鱼(Carassius auratus)中的驱虫作用及其3D-QSAR分析

三代虫属。是常见的单基因外寄生物,可能导致大量鱼类死亡。要查找与低毒性有效的驱虫剂,获得了一系列的天然皂苷,并评估它们对驱虫活性三代虫kobayashii和急性毒性金鱼(鲫鱼)。在所有测试的化合物中,六个化合物(1、2、3、8、10和13)显示出比广泛使用的基于甲醛的寄生虫杀虫剂更高的驱虫活性和安全性,尤其是化合物1对小林种的驱虫效果为100%剂量为0.3 mg / L,治疗指数为16.6。此外,已经执行了这些皂甙的三维定量构效关系(3D-QSAR)研究以探索合理靠在驱虫活性的结构特征G. kobayashii。这些模型表明C-17位的羟基和C-3位的糖部分,特别是糖部分的羟基,对驱虫活性至关重要。QSAR研究可为进一步合理设计和优化新型皂苷控制回旋肌病提供有用的信息。

更新日期:2021-01-10
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