Natural Chemistry Research Group, Department of Chemistry, University of Turku, FI-20014 Turku, Finland.
UMR 1225 IHAP, INRAE/ENVT, 23 Chemin des Capelles, 31076 Toulouse Cedex, France.
J Agric Food Chem. 2020 Apr 8;68(14):4176-4186. doi: 10.1021/acs.jafc.9b06774. Epub 2020 Mar 26.
Worldwide, parasitic gastrointestinal nematodes continue to threaten animal health, welfare, and production in outdoor breeding systems of small ruminants. For more than 50 years, the control of these parasitic worms has relied on the use of commercial synthetic anthelmintics. However, anthelmintic resistance in worm populations is nowadays widespread and requires novel solutions. The use of tannin-rich plants has been suggested as an alternative to synthetic anthelmintics to control gastrointestinal nematodes. The majority of previous studies have focused on the activity of proanthocyanidins (syn condensed tannins), and less is known about ellagitannins. In this study, the effects of 30 structurally unique ellagitannins on the exsheathment of third-stage infective larvae were examined on and by the in vitro larval exsheathment inhibition assay. Ellagitannins were found to be promising natural anthelmintics as they showed direct inhibition on larval exsheathment for both nematode species. In general, ellagitannins were more efficient at inhibiting the exsheathment of larvae than those of . The efficiency of inhibition increased as the degree of oligomerization or the molecular weight of the ellagitannin increased. Otherwise, we found no other structural features of ellagitannins that significantly affected the anthelmintic activity on the third-stage infective larvae. The effective concentrations were physiologically relevant and should be achievable in the gastrointestinal tract also in in vivo conditions.
在全球范围内,寄生性胃肠道线虫继续威胁着户外饲养小反刍动物系统中的动物健康、福利和生产。50 多年来,这些寄生虫的控制一直依赖于商业合成驱虫药的使用。然而,如今蠕虫种群中的驱虫剂耐药性广泛存在,需要新的解决方案。人们已经提出使用富含单宁的植物作为合成驱虫剂的替代品来控制胃肠道线虫。以前的大多数研究都集中在原花青素(即缩合单宁)的活性上,而对鞣花单宁知之甚少。在这项研究中,通过体外幼虫蜕皮抑制试验,检查了 30 种结构独特的鞣花单宁对第三期感染性幼虫蜕皮的影响。鞣花单宁被认为是很有前途的天然驱虫药,因为它们对两种线虫都表现出直接抑制幼虫蜕皮的作用。一般来说,鞣花单宁对 幼虫蜕皮的抑制效率高于 幼虫。随着鞣花单宁聚合度或分子量的增加,抑制效率也随之增加。此外,我们没有发现鞣花单宁的其他结构特征会显著影响对第三期感染性幼虫的驱虫活性。有效浓度在生理上是相关的,在体内条件下也应该能够在胃肠道中达到。