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通过实验和计算机辅助机制深入了解 Dita 树皮的先导生物活性分离物的药理学作用及预测。

Pharmacological insights and prediction of lead bioactive isolates of Dita bark through experimental and computer-aided mechanism.

机构信息

Department of Pharmacy, International Islamic University Chittagong, Chittagong, 4318, Bangladesh.

Biomedical and Toxicological Research Institute, Bangladesh Council of Scientific and Industrial Research, Dhaka, 1205, Bangladesh.

出版信息

Biomed Pharmacother. 2020 Nov;131:110774. doi: 10.1016/j.biopha.2020.110774. Epub 2020 Oct 5.

Abstract

Dita bark (Alstonia scholaris (L.) R. Br.) is an ethnomedicine used for the management of various ailments. This study aimed to investigate the biological properties of methanol extract of A. scholaris bark (MEAS), through in vivo, in vitro and in silico approaches alongside its phytochemical profiling. Identification and nature of the bioactive secondary metabolites were studied by the established qualitative tests and GC-MS analysis. The antidepressant activity was determined by forced swimming test (FST) and tail suspension test (TST) in mice. The anti-inflammatory and thrombolytic effect was evaluated using inhibition of protein denaturation technique and clot lysis technique, respectively. Besides, computational studies of the isolated compounds and ADME/T analysis were performed by Schrödinger-Maestro (v11.1) software, and PASS prediction was conducted through PASS online tools. The GC-MS analysis revealed the presence of several secondary metabolites in MEAS. Treatment with MEAS revealed a significant reduction of immobility time in a dose-dependent manner in FST and TST. Besides, MEAS showed substantial anti-inflammatory effects at the higher dose (400 μg/mL) as well as revealed notable clot lysis effect as compared to control. In the case of computer-aided investigation, all compounds meet the condition of Lipinski's rule of five. PASS study also predicted for all compounds, and among these safe compound furazan-3-amine showed the most spontaneous binding energy for both antidepressant and thrombolytic activities, as well as 5-dimethylamino-6 azauracil, found promising for anti-inflammatory activity. Taken together, the investigation concludes that MEAS can be a potent source of antidepressant, anti-inflammatory, and thrombolytic agents.

摘要

棣棠叶(Alstonia scholaris(L.)R. Br.)是一种被广泛应用于治疗多种疾病的民族药物。本研究旨在通过体内、体外和计算方法,结合其植物化学分析,研究棣棠叶甲醇提取物(MEAS)的生物特性。通过建立的定性试验和 GC-MS 分析,鉴定和确定生物活性次生代谢物的性质。通过强迫游泳试验(FST)和悬尾试验(TST)在小鼠中确定抗抑郁活性。采用抑制蛋白变性技术和血栓溶解技术分别评估抗炎和溶栓作用。此外,通过 Schrödinger-Maestro(v11.1)软件对分离化合物进行计算研究和 ADME/T 分析,并通过 PASS 在线工具进行 PASS 预测。GC-MS 分析表明 MEAS 中存在多种次生代谢物。MEAS 的治疗在 FST 和 TST 中以剂量依赖性方式显著减少了不动时间。此外,MEAS 在较高剂量(400μg/mL)下表现出显著的抗炎作用,并且与对照组相比,显示出明显的血栓溶解作用。在计算机辅助研究的情况下,所有化合物都符合 Lipinski 五规则。PASS 研究还预测了所有化合物,其中安全化合物呋喃-3-胺在抗抑郁和溶栓活性方面表现出最自发的结合能,5-二甲基氨基-6-氮杂尿嘧啶在抗炎活性方面也表现出了很大的潜力。综上所述,本研究表明 MEAS 可能是一种有效的抗抑郁、抗炎和溶栓药物的潜在来源。

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