黄菖蒲根茎水醇提取物及其成分的体内抗疟活性。
In vivo anti-malarial activity of the hydroalcoholic extract of rhizomes of Kniphofia foliosa and its constituents.
机构信息
Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, College of Health Sciences, Addis Ababa University, Addis Ababa, Ethiopia.
出版信息
Malar J. 2021 Jan 1;20(1):3. doi: 10.1186/s12936-020-03552-7.
BACKGROUND
Kniphofia foliosa is a flamboyant robust perennial herb which has dense clumps and tick upright rhizomes with leaves at the base. In Ethiopia, it has several vernacular names including Abelbila, Ashenda, Amelmela, Yeznjero Ageda, Shemetmetie and Yezinjero Ageda. The plant is endemic to Ethiopian highlands, where its rhizomes are traditionally used for the treatment of malaria, abdominal cramps and wound healing. In the present study, the 80% methanol extract of K. foliosa rhizomes and its constituents are tested against Plasmodium berghei in mice.
METHODS
Isolation was carried out using column and preparative thin layer chromatography (PTLC). The chemical structures of the compounds were elucidated by spectroscopic methods (ESI-MS, 1D and 2D-NMR). Peters' 4-day suppressive test against P. berghei in mice was utilized for in vivo anti-malarial evaluation of the test substances.
RESULTS
Two compounds, namely knipholone and dianellin were isolated from the 80% methanolic extract of K. foliosa rhizomes, and characterized. The hydroalcoholic extract (400 mg/kg) and knipholone (200 mg/kg) showed the highest activity with chemosuppression values of 61.52 and 60.16%, respectively. From the dose-response plot, the median effective (ED) doses of knipholone and dianellin were determined to be 81.25 and 92.31 mg/kg, respectively. Molecular docking study revealed that knipholone had a strong binding affinity to Plasmodium falciparum l-lactate dehydrogenase (pfLDH) target.
CONCLUSION
Results of the current study support the traditional use of the plant for the treatment of malaria.
背景
火鹤花是一种绚丽多姿的多年生草本植物，具有茂密的丛生和直立的根茎，基部有叶子。在埃塞俄比亚，它有几个土名，包括 Abelbila、Ashenda、Amelmela、Yeznjero Ageda、Shemetmetie 和 Yezinjero Ageda。该植物是埃塞俄比亚高地的特有种，其根茎传统上用于治疗疟疾、腹痛和伤口愈合。在本研究中，火鹤花根茎的 80%甲醇提取物及其成分在小鼠中被测试对疟原虫的作用。
方法
使用柱层析和制备薄层层析（PTLC）进行分离。通过光谱方法（ESI-MS、1D 和 2D-NMR）阐明化合物的化学结构。利用彼得斯氏 4 天抑制试验对小鼠体内的抗疟活性进行了测试。
结果
从火鹤花根茎的 80%甲醇提取物中分离出两种化合物，即 knipholone 和 dianellin，并进行了表征。水醇提取物（400mg/kg）和 knipholone（200mg/kg）表现出最高的活性，化学抑制率分别为 61.52%和 60.16%。从剂量反应图中，确定 knipholone 和 dianellin 的半数有效剂量（ED）分别为 81.25 和 92.31mg/kg。分子对接研究表明，knipholone 与恶性疟原虫 l-乳酸脱氢酶（pfLDH）靶标具有很强的结合亲和力。
结论
本研究结果支持该植物用于治疗疟疾的传统用途。
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