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抗盘尾丝虫和抗线虫活性的一个水醇提自 Acacia nilotica 的果实和一些原花青素衍生物。

Anti-Onchocerca and Anti-Caenorhabditis Activity of a Hydro-Alcoholic Extract from the Fruits of Acacia nilotica and Some Proanthocyanidin Derivatives.

机构信息

Department of Biological Sciences, Faculty of Science, University of Ngaoundere, P.O. Box 454, Ngaoundere, Cameroon.

Institute of Pharmaceutical Biology and Phytochemistry (IPBP), University of Münster, PharmaCampus Correnstrasse 48, D-48149 Münster, Germany.

出版信息

Molecules. 2017 May 6;22(5):748. doi: 10.3390/molecules22050748.

Abstract

fruits with high tannin content are used in the northern parts of Cameroon as anti-filarial remedies by traditional healers. In this study, the hydro-alcoholic fruit extract (crude extract (CE)) and, one of the main constituents in its most active fractions, (+)-catechin-3--gallate (CG), as well as four related proanthocyanidins, (-)-epicatechin-3--gallate (ECG), (+)-gallocatechin (GC), (-)-epigallocatechin (EGC) and (-)-epigallocatechin-3--gallate (EGCG), were assessed for their potential in vitro anthelmintic properties against the free-living model organism and against the cattle filarial parasite . Worms were incubated in the presence of different concentrations of fruit extract, fractions and pure compounds. The effects on mortality were monitored after 48 h. The plant extract and all of the pure tested compounds were active against (LC ranging from 1.2 to 11.5 µg/mL on males) and (LC ranging from 33.8 to 350 µg/mL on wild type). While high LC were required for the effects of the compounds on , very low LC were required against . Importantly, tests for acute oral toxicity (lowest dose: 10 mg/kg) in Wistar rats demonstrated that crude extract and pure compounds were non-toxic and safe to use. Additionally, the results of cytotoxicity tests with the Caco-2 cell line (CC ranging from 47.1 to 93.2 µg/mL) confirmed the absence of significant toxicity of the crude extract and pure compounds. These results are in good accordance with the use of against nematode infections by traditional healers, herdsmen and pastoralists in Cameroon.

摘要

在喀麦隆北部,传统的治疗师使用单宁含量高的水果作为抗丝虫病的药物。在这项研究中,评估了水醇水果提取物(粗提物(CE))及其最活跃部分之一的(+)-儿茶素-3--没食子酸酯(CG),以及四种相关的原花青素,(-)-表儿茶素-3--没食子酸酯(ECG)、(+)-没食子儿茶素(GC)、(-)-表儿茶素(EGC)和(-)-表儿茶素-3--没食子酸酯(EGCG)在体外对抗自由生活模式生物和牛丝状寄生虫的潜在驱虫特性。将蠕虫在不同浓度的果实提取物、馏分和纯化合物中孵育。48 小时后监测死亡率的影响。植物提取物和所有测试的纯化合物都对(LC 范围为 1.2 至 11.5 µg/mL,雄性)和(野生型 LC 范围为 33.8 至 350 µg/mL)有效。虽然化合物对的作用需要高 LC,但对的作用需要非常低的 LC。重要的是,用 Wistar 大鼠进行的急性口服毒性试验(最低剂量:10 mg/kg)表明,粗提物和纯化合物均无毒性,使用安全。此外,Caco-2 细胞系的细胞毒性试验结果(CC 范围为 47.1 至 93.2 µg/mL)证实了粗提物和纯化合物没有明显的毒性。这些结果与喀麦隆传统治疗师、牧民和牧民使用来治疗线虫感染是一致的。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/aab4/6154738/58edee8cd184/molecules-22-00748-g001.jpg

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