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来自喀麦隆番荔枝科的强效抗疟提取物。

Potent antiplasmodial extracts from Cameroonian Annonaceae.

机构信息

Laboratory of Phytobiochemistry and Medicinal Plants Study, Faculty of Science, University of Yaoundé I, P.O. Box 812, Yaoundé, Cameroon.

出版信息

J Ethnopharmacol. 2011 Apr 12;134(3):717-24. doi: 10.1016/j.jep.2011.01.020. Epub 2011 Jan 21.

Abstract

AIM OF THE STUDY

In a search for new antimalarial leads, we have carried out a preliminary ethnopharmacological study with the aim of evaluating the in vitro antiplasmodial activity of extracts from thirteen Annonaceae species growing in Cameroon, and of assessing the acute toxicity of promising fractions in Swiss albino mice.

MATERIALS AND METHODS

Plants were selected on the basis of an ethnobotanical survey carried out in four sites in centre and south regions of Cameroon (Yaoundé neighbourhoods, Kon-Yambetta, Ngobayang and Mbalmayo) on Annonaceae plants locally used to treat malaria and related symptoms. The choice of the sites was mainly based on environmental factors enabling mosquito breeding, cosmopolitan areas regrouping people from different cultural origins, areas with limited access to health centers, and areas with people relying exclusively on traditional medical practices. Collected materials were extracted by maceration in 95% ethanol. The crude extract was partitioned using organic solvents and the fractions afforded were evaluated for antiplasmodial activity in culture against the W2 strain of Plasmodium falciparum. Promising fractions (methanol fractions) were assessed for their acute toxicity in Swiss albino mice.

RESULTS

From the results achieved, 37 (31.3%) out of 118 extracts tested exhibited antiplasmodial activity, with IC(50) values ranging from 1.07 μg/ml to 9.03 μg/ml. Of the active extracts, 29 (78.4%) were methanol fractions, 21 (72.4%) of which inhibited the parasites with IC(50)<5 μg/ml. The promising fractions proved to be safe through oral administration in mice.

CONCLUSIONS

The activities and toxicity profiles of methanol fractions indicate that they deserve to be further investigated in detail for antimalarial lead discovery.

摘要

研究目的

在寻找新的抗疟先导化合物的过程中,我们进行了一项初步的民族药理学研究,旨在评估 13 种生长在喀麦隆的番荔枝科植物提取物的体外抗疟活性,并评估有前途的部分在瑞士白化病小鼠中的急性毒性。

材料和方法

根据在喀麦隆中部和南部四个地区(雅温得附近地区、科恩-雅贝塔、恩戈巴扬和姆巴梅约)进行的民族植物学调查,选择植物来治疗疟疾和相关症状。选择这些地点的主要依据是有利于蚊子繁殖的环境因素、汇集不同文化起源人群的世界性地区、获得卫生中心机会有限的地区以及完全依赖传统医学实践的人群地区。收集的材料用 95%乙醇进行浸提。粗提取物用有机溶剂进行分配,评估抗疟活性在培养物中对恶性疟原虫 W2 株的活性。对有前途的部分(甲醇部分)在瑞士白化病小鼠中进行了急性毒性评估。

结果

在所获得的结果中,118 种测试提取物中有 37 种(31.3%)表现出抗疟活性,IC50 值范围为 1.07μg/ml 至 9.03μg/ml。在活性提取物中,有 29 种(78.4%)是甲醇部分,其中有 21 种(72.4%)的 IC50<5μg/ml 抑制寄生虫。通过口服给药,有前途的部分在小鼠中被证明是安全的。

结论

甲醇部分的活性和毒性谱表明,它们值得进一步详细研究,以发现抗疟先导化合物。

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