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从铺地黍(Wall ex. Duby)中分离得到的山奈酚衍生物诱导瑞利绦虫乙酰胆碱酯酶和一氧化氮合酶的改变。

A kaempferol derivative isolated from Lysimachia ramosa (Wall ex. Duby) induced alteration of acetyl cholinesterase and nitric oxide synthase in Raillietina echinobothrida.

机构信息

Parasitology Laboratory, Department of Zoology, North-Eastern Hill University, Shillong, 793022, India.

Parasitology Laboratory, Department of Zoology, North-Eastern Hill University, Shillong, 793022, India.

出版信息

Vet Parasitol. 2021 Aug;296:109461. doi: 10.1016/j.vetpar.2021.109461. Epub 2021 Jun 18.

DOI:10.1016/j.vetpar.2021.109461
PMID:34214945
Abstract

Lysimachia ramosa has been used as a traditional medicine among the tribal population of Meghalaya, northeast India, for the control of helminthosis. The anthelmintic efficacy of L. ramosa has been documented earlier. In the present study, the active compound from L. ramosa has been isolated and identified using mass and NMR spectra. It's in vitro anthelmintic activity was evaluated against Raillietina echinobothrida, one of the most pathogenic cestode of domestic fowl. The isolated active compound was characterized to be a kaempferol derivative which showed potent anthelmintic activity against R. echinobothrida by changing surface ultrastructure and also inhibiting the activity of two neurotransmitter enzymes: acetyl cholinesterase (AChE) and nitric oxide synthase (NOS), both of which are known to perform dynamic roles in the intracellular communication mediated through neuromuscular system. Motility reduction, deformation in the surface architecture, extensive ultrastructural alterations and reduced histochemical stain intensity in both AChE and NOS was observed in the treated parasites. Biochemical result also revealed alteration in the enzyme activities in the treated parasites. Further, depletion in the nitric oxide (NO) production in the bioactive component exposed tissues of R. echinobothrida was also detected. The results provided evidence that the bioactive compound could be further explored to control helminthosis at a large scale.

摘要

鸡冠状犁头草被印度东北部梅加拉亚邦的部落居民用作一种传统药物,以控制寄生虫病。此前已有研究证明鸡冠状犁头草具有驱虫功效。在本研究中,使用质谱和 NMR 光谱对鸡冠状犁头草中的活性化合物进行了分离和鉴定。该活性化合物对瑞利绦虫(一种对家禽最具致病性的绦虫)的体外驱虫活性进行了评估。分离出的活性化合物被鉴定为山奈酚衍生物,它通过改变表面超微结构,以及抑制两种神经递质酶(乙酰胆碱酯酶(AChE)和一氧化氮合酶(NOS))的活性,对瑞利绦虫表现出很强的驱虫活性,这两种酶都在通过神经肌肉系统介导的细胞内通讯中发挥动态作用。在处理过的寄生虫中,观察到运动能力下降、表面结构变形、广泛的超微结构改变以及 AChE 和 NOS 的组织化学染色强度降低。生化结果还表明,处理过的寄生虫中的酶活性发生了改变。此外,还检测到瑞利绦虫暴露于活性化合物的组织中一氧化氮(NO)生成减少。这些结果为该生物活性化合物可进一步用于大规模控制寄生虫病提供了证据。

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