通过体内、体外和计算机模拟方法研究 var. (D.Don) & Mondal 叶的生物活性和生物活性成分的特性。

Investigation of the Biological Activities and Characterization of Bioactive Constituents of var. (D.Don) & Mondal Leaves through In Vivo, In Vitro, and In Silico Approaches.

机构信息

Department of Bio-Health Technology, Kangwon National University, Chuncheon 24341, Korea.

Senior Scientist, Rentia Plant Factory, Chuncheon 24341, Korea.

出版信息

Molecules. 2019 Apr 8;24(7):1367. doi: 10.3390/molecules24071367.

Abstract

var. is one of the most frequently used ethnomedicinal plants by the indigenous communities of Bangladesh. This study was designed to investigate the antidiarrheal, anti-inflammatory, anthelmintic and antibacterial activities of the ethanol extract of leaves (EEOR). The leaves were extracted with ethanol and subjected to in vivo antidiarrheal screening using the castor oil-induced diarrhea, enteropooling, and gastrointestinal transit models. Anti-inflammatory efficacy was evaluated using the histamine-induced paw edema test. In parallel, in vitro anthelmintic and antibacterial activities were evaluated using the aquatic worm and disc diffusion assays respectively. In all three diarrheal models, EEOR (100, 200 and 400 mg/kg) showed obvious inhibition of diarrheal stool frequency, reduction of the volume and weight of the intestinal contents, and significant inhibition of intestinal motility. Also, EEOR manifested dose-dependent anti-inflammatory activity. Anthelmintic action was deemed significant ( < 0.001) with respect to the onset of paralysis and helminth death. EEOR also resulted in strong zones of inhibition when tested against both Gram-positive and Gram-negative bacteria. GC-MS analysis identified 30 compounds within EEOR, and of these, 13 compounds documented as bioactive showed good binding affinities to M3 muscarinic acetylcholine, 5-HT3, tubulin and GlcN-6-P synthase protein targets in molecular docking experiments. Additionally, ADME/T and PASS analyses revealed their drug-likeness, likely safety upon consumption and possible pharmacological activities. In conclusion, our findings scientifically support the ethnomedicinal use and value of this plant, which may provide a potential source for future development of medicines.

摘要

var. 是孟加拉国土著社区最常使用的药用植物之一。本研究旨在研究 叶乙醇提取物(EEOR)的抗腹泻、抗炎、驱虫和抗菌活性。将叶片用乙醇提取,并通过蓖麻油诱导的腹泻、肠液积聚和胃肠转运模型进行体内抗腹泻筛选。使用组胺诱导的爪肿胀试验评估抗炎功效。同时,使用水蠕虫和圆盘扩散试验分别评估体外驱虫和抗菌活性。在所有三种腹泻模型中,EEOR(100、200 和 400 mg/kg)均明显抑制腹泻粪便频率、减少肠道内容物的体积和重量,并显著抑制肠道蠕动。此外,EEOR表现出剂量依赖性抗炎活性。驱虫作用被认为是显著的(<0.001),与瘫痪和寄生虫死亡的开始有关。EEOR 对革兰氏阳性和革兰氏阴性菌也表现出强烈的抑制区。GC-MS 分析确定 EEOR 中有 30 种化合物,其中 13 种被证明具有生物活性的化合物在分子对接实验中与 M3 毒蕈碱乙酰胆碱、5-HT3、微管蛋白和 GlcN-6-P 合酶蛋白靶标具有良好的结合亲和力。此外,ADME/T 和 PASS 分析表明它们具有药物样特性、可能在消费时安全且可能具有药理学活性。总之,我们的研究结果从科学上支持了这种植物的民族医学用途和价值,它可能为未来药物的开发提供潜在的来源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a86a/6480688/5df3c848c993/molecules-24-01367-g001.jpg

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