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抗盘尾丝虫活性及节节草精油的植物化学分析

Anti-Onchocerca activity and phytochemical analysis of an essential oil from Cyperus articulatus L.

机构信息

ANDI Centre of Excellence, Biotechnology Unit, Faculty of Science, University of Buea, P,O, Box 63, Buea, Cameroon.

出版信息

BMC Complement Altern Med. 2014 Jul 7;14:223. doi: 10.1186/1472-6882-14-223.

Abstract

BACKGROUND

The lack of a safe and effective adult worm drug and the emergence of resistant animal parasite strains to the only recommended drug, the microfilaricide, ivermectin put many at risk of the devastating effects of the onchocerciasis. The present study was undertaken to investigate the acclaimed anti-Onchocerca activity of the roots/rhizomes of Cyperus articulatus in the traditional treatment of onchocerciasis in North Western Cameroon and to assess the plant as a new source of potential filaricidal lead compounds.

METHODS

Crude extracts were prepared from the dried plant parts using hexane, methylene chloride and methanol. The antifilarial activity was evaluated in vitro on microfilariae (Mfs) and adult worms of the bovine derived Onchocerca ochengi, a close relative of Onchocerca volvulus. The viabilities of microfilariae and adult male worms were determined based on motility reduction, while for the adult female worms the viability was based on the standard MTT/formazan assay. Cytotoxicity of the active extract was assessed on monkey kidney epithelial cells in vitro and the selectivity indices (SI) were determined. Acute toxicity of the promising extract was investigated in mice. Chemical composition of the active extract was unraveled by GC/MS analysis.

RESULTS

Only the hexane extract, an essential oil exhibited anti-Onchocerca activity. The oil killed both the microfilariae and adult worms of O. ochengi in a dose manner dependently, with IC50s of 23.4 μg/ml on the Mfs, 23.4 μg/ml on adult male worms and 31.25 μg/ml on the adult female worms. Selectivity indices were 4, 4, and 2.99 for Mfs, adult males and adult females, respectively. At a single limit dose of 2000 mg/kg body weight, none of 6 mice that received the essential oil by gavage died. GC/MS analysis revealed the presence of terpenoids, hydrocarbons and fatty acids or fatty acid derivatives as components of the oil.

CONCLUSIONS

The essential oil from the roots/rhizomes of Cyperus articulatus is active against O. ochengi microfilariae and adult worms in vitro in a dose dependent manner, hence may provide a source of new anti-filarial compounds. The results also support the traditional use of C. articulatus in the treatment of human onchocerciasis.

摘要

背景

缺乏安全有效的成虫药物,以及唯一推荐的药物——微丝蚴杀虫剂伊维菌素对动物寄生虫株的抗药性,使许多人面临盘尾丝虫病毁灭性影响的风险。本研究旨在调查在西北喀麦隆传统治疗盘尾丝虫病中,莎草科莎草属根茎被称赞的抗盘尾丝虫活性,并评估该植物作为新的潜在杀丝蚴先导化合物的来源。

方法

使用正己烷、二氯甲烷和甲醇从干燥的植物部分制备粗提取物。在体外,用微丝蚴(Mfs)和牛源性盘尾丝虫成虫(一种与旋盘尾丝虫密切相关的寄生虫)评估抗丝虫活性。根据运动减少来确定微丝蚴和雄性成虫的存活率,而对于雌性成虫,则根据标准 MTT/甲瓒测定法来确定存活率。在体外评估活性提取物对猴肾上皮细胞的细胞毒性,并确定选择性指数(SI)。在小鼠中研究有希望的提取物的急性毒性。通过 GC/MS 分析揭示活性提取物的化学成分。

结果

只有正己烷提取物(一种精油)表现出抗盘尾丝虫活性。该油以剂量依赖性方式杀死 O.ochengi 的微丝蚴和成虫,微丝蚴的 IC50 为 23.4μg/ml,雄性成虫为 23.4μg/ml,雌性成虫为 31.25μg/ml。对微丝蚴、雄性成虫和雌性成虫的选择性指数分别为 4、4 和 2.99。在单次限制剂量为 2000mg/kg 体重时,接受灌胃的精油的 6 只小鼠均未死亡。GC/MS 分析显示,该油的成分包括萜类化合物、碳氢化合物和脂肪酸或脂肪酸衍生物。

结论

莎草科莎草属根茎的精油对 O.ochengi 的微丝蚴和成虫在体外具有剂量依赖性的活性,因此可能为新的抗丝虫化合物提供来源。研究结果也支持莎草属在治疗人类盘尾丝虫病中的传统用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c935/4099029/7149d368a507/1472-6882-14-223-1.jpg

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