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采用实验和计算方法研究 叶的潜在抗氧化、溶栓和神经药理学活性。

Investigation of Potential Antioxidant, Thrombolytic and Neuropharmacological Activities of Leaves Using Experimental and In Silico Approaches.

机构信息

Department of Biomedical Science, School of Medicine, Brain Science and Engineering Institute, Kyungpook National University, Daegu 41944, Korea.

Department of Pharmacology, School of Medicine, Brain Science and Engineering Institute, Kyungpook National University, Daegu 41944, Korea.

出版信息

Molecules. 2021 Feb 12;26(4):975. doi: 10.3390/molecules26040975.

Abstract

The leaves of are traditionally used in Bangladesh for the treatment of different chronic ailments. The purpose of this study was to explore in vitro antioxidant, thrombolytic activities, and in vivo neuropharmacological effects of methanolic extract of (MEHA) leaves. Antioxidant activity of MEHA was assessed by a DPPH free radical scavenging assay and total phenolics content, total flavonoids content were also measured. The thrombolytic activity was determined by percentage of clot lysis and neuropharmacological activities by hole board, tail suspension, forced swimming and elevated plus maze tests. The results showed that the IC value of the extract against DPPH was 199.51 μg/mL. Quantitative analysis displayed higher contents of phenolics and flavonoids (147.71 mg gallic acid equivalent/g & 66.65 mg quercetin equivalent/g dried extract, respectively). The extract also showed a significant clot lysis (33.31%) activity. In case of anxiolytic activity, the elevate plus maze (EPM) test demonstrated an increase in time spent in open arms, and in case of hole board test, the number of head dipping was also significantly increased ( < 0.05). All the test compared with control (1% Tween in water) and standard (diazepam 1 mg/kg), significant dose (200 & 400 mg/kg) dependent anxiolytic activity was found. In antidepressant activity, there was a significant decrease in period of immobility in both test models (tail suspension and forced swimming) ( < 0.05). Moreover, 13 compounds were identified as bioactive, showed good binding affinities to xanthine oxidoreductase, tissue plasminogen activator receptor, potassium channel receptor, human serotonin receptor targets in molecular docking experiments. Furthermore, ADME/T analysis revealed their drug-likeness, likely pharmacological actions and non-toxic upon consumption. Taken together, our finding support the traditional medicinal use of this plant, which may provide a potential source for future drug discovery.

摘要

的叶子在孟加拉国传统上被用于治疗各种慢性疾病。本研究旨在探索 的甲醇提取物 (MEHA) 叶子的体外抗氧化、溶栓活性和体内神经药理学作用。通过 DPPH 自由基清除测定法和总酚含量、总黄酮含量来评估 MEHA 的抗氧化活性。溶栓活性通过凝块溶解百分比来确定,神经药理学活性通过洞板、悬尾、强迫游泳和高架十字迷宫试验来确定。结果表明,该提取物对 DPPH 的 IC 值为 199.51μg/mL。定量分析显示出更高的酚类和类黄酮含量(分别为 147.71 毫克没食子酸当量/g 和 66.65 毫克槲皮素当量/g 干提取物)。该提取物还显示出显著的凝块溶解(33.31%)活性。在抗焦虑活性方面,高架十字迷宫(EPM)试验显示出在开放臂中花费的时间增加,而在洞板试验中,头浸次数也显著增加( < 0.05)。所有测试均与对照(水中 1%吐温)和标准(地西泮 1mg/kg)进行比较,发现具有显著的剂量(200 和 400mg/kg)依赖性抗焦虑活性。在抗抑郁活性方面,两种测试模型(悬尾和强迫游泳)中不动期都有显著减少( < 0.05)。此外,在分子对接实验中,有 13 种化合物被鉴定为具有生物活性的化合物,对黄嘌呤氧化还原酶、组织纤溶酶原激活物受体、钾通道受体、人 5-羟色胺受体靶点显示出良好的结合亲和力。此外,ADME/T 分析表明它们具有药物样性质、可能的药理作用和在摄入后无毒性。综上所述,我们的发现支持这种植物的传统药用价值,这可能为未来的药物发现提供一个潜在的来源。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/191e/7918836/5e31d2be5cde/molecules-26-00975-g001.jpg

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