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来自木犀科女贞亚属粗提物、溶剂提取物及薄层层析分离化合物的抗疟活性评价

Antimalarial Evaluation of Crude Extract, Solvent Fractions, and TLC-Isolated Compounds from Linn subsp. (Oleaceae).

作者信息

Hailesilase Gebretekle Gebremichael, Rajeshwar Yarra, Hailu Gebremedhin Solomon, Sibhat Gereziher Gebremedhin, Bitew Helen

机构信息

Department of Pharmacy, Adigrat University, Adigrat, Ethiopia.

Department of Medicinal Chemistry, Mekelle University, Mekelle, Ethiopia.

出版信息

Evid Based Complement Alternat Med. 2020 May 13;2020:6731485. doi: 10.1155/2020/6731485. eCollection 2020.

Abstract

Malaria is a major global public health problem caused by parasites. Drug resistance is becoming a great challenge. New drugs with novel mechanism of action are urgently required. In malarious countries, medicinal plants are commonly used for malaria treatment. is traditionally used against malaria in Ethiopia. The aim of this study was to isolate and evaluate antimalarial activity of chemical constituents extracted from against chloroquine-sensitive -infected mice. Stem bark of was extracted with 80% methanol and fractionated with three solvents. The butanol fraction was subjected to isolation with preparative thin-layer chromatography (PTLC). Acute oral toxicity studies were conducted in mice as per the Organization for Economic Co-operation and Development (OECD) guideline 425. Antimalarial activities of the test substances were evaluated using Peter's 4-day suppressive test. The crude extract showed significant ( < 0.01) antiplasmodial activity at all doses with a chemosuppression value of 52.40% at a dose of 600 mg/kg. All fractions also suppressed parasitaemia significantly ( < 0.05), the highest suppression (45.42%) being with butanol fraction. In the phytochemical analysis, two compounds were isolated. Both compounds showed significant ( < 0.05) antimalarial activities. Compound C inhibited parasitaemia up to 38.19% at a dose of 200 mg/kg. The crude extract, butanol fraction, and isolated compounds also prolonged survival time of mice. No sign of toxicity and mortality was seen in the test substances at up to a single dose of 2 g/kg. Findings of the current study may confirm the traditional antimalarial claim of and its relative safety as well as the potentiality of compound C for further investigations.

摘要

疟疾是由寄生虫引起的一个重大全球公共卫生问题。耐药性正成为一个巨大挑战。迫切需要具有新型作用机制的新药。在疟疾流行国家,药用植物通常用于疟疾治疗。在埃塞俄比亚,[植物名称未给出]传统上用于治疗疟疾。本研究的目的是分离并评估从[植物名称未给出]中提取的化学成分对氯喹敏感的[寄生虫名称未给出]感染小鼠的抗疟活性。[植物名称未给出]的茎皮用80%甲醇提取,并用三种溶剂进行分馏。正丁醇馏分通过制备薄层色谱法(PTLC)进行分离。按照经济合作与发展组织(OECD)指南425在小鼠中进行急性经口毒性研究。使用彼得4天抑制试验评估受试物质的抗疟活性。粗提物在所有剂量下均显示出显著(<0.01)的抗疟原虫活性,在600mg/kg剂量下化学抑制值为52.40%。所有馏分也均显著抑制(<0.05)寄生虫血症,最高抑制率(45.42%)出现在正丁醇馏分中。在植物化学分析中,分离出两种化合物。两种化合物均显示出显著(<0.05)的抗疟活性。化合物C在200mg/kg剂量下抑制寄生虫血症高达38.19%。粗提物、正丁醇馏分和分离出的化合物也延长了小鼠的存活时间。在高达2g/kg的单剂量下,受试物质未观察到毒性和死亡迹象。本研究结果可能证实了[植物名称未给出]的传统抗疟说法及其相对安全性以及化合物C进一步研究的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/466c/7244953/ff48c5725d8c/ECAM2020-6731485.001.jpg

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