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采用实验和计算方法揭示叶的生物活性。

Unravelling the Biological Activities of the Leaves Using Experimental and Computational Approaches.

机构信息

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

Department of Theoretical and Computational Chemistry, University of Dhaka, Dhaka 1000, Bangladesh.

出版信息

Molecules. 2020 Oct 15;25(20):4737. doi: 10.3390/molecules25204737.

Abstract

is locally known as Harijora, and used by the native hill-tract people of Bangladesh for the treatment of rheumatalgia, snake bite, syphilis, fractured bones, elephantiasis and an antidote for poisoning. The present study was carried out to determine the possible anti-inflammatory, analgesic, neuropharmacological and anti-diarrhoeal activity of the methanol extract of leaves (MEBPL) through in vitro, in vivo and in silico approaches. In the anti-inflammatory study, evaluated by membrane stabilizing and protein denaturation methods, MEBPL showed a significant and dose dependent inhibition. The analgesic effect of MEBPL tested by inducing acetic acid and formalin revealed significant inhibition of pain in both tests. During the anxiolytic evaluation, the extract exhibited a significant and dose-dependent reduction of anxiety-like behaviour in mice. Similarly, mice treated with MEBPL demonstrated dose-dependent reduction in locomotion effect in the open field test and increased sedative effect in the thiopental sodium induced sleeping test. MEBPL also showed good anti-diarrheal activity in both castor oil induced diarrheal and intestinal motility tests. Besides, a previously isolated compound (beta-sitosterol) exhibited good binding affinity in docking and drug-likeliness properties in ADME/T studies. Overall, is a biologically active plant and could be a potential source of drug leads, which warrants further advanced study.

摘要

它在当地被称为 Harijora,被孟加拉国的本地山地部落人民用于治疗风湿病、蛇咬伤、梅毒、骨折、象皮病和中毒解毒。本研究通过体外、体内和计算机模拟方法,研究了 leaves 的甲醇提取物 (MEBPL) 可能的抗炎、镇痛、神经药理学和抗腹泻活性。在通过膜稳定和蛋白质变性方法评估的抗炎研究中,MEBPL 表现出显著的、剂量依赖性的抑制作用。通过诱导乙酸和甲醛来测试 MEBPL 的镇痛作用,结果表明在两种测试中都显著抑制了疼痛。在焦虑评估中,提取物在小鼠中表现出明显的、剂量依赖性的焦虑样行为减少。同样,用 MEBPL 治疗的小鼠在旷场试验中表现出运动效应的剂量依赖性降低,在戊巴比妥钠诱导的睡眠试验中表现出镇静作用的增加。MEBPL 在蓖麻油诱导的腹泻和肠道运动试验中也显示出良好的抗腹泻活性。此外,先前分离的化合物(β-谷甾醇)在对接和 ADME/T 研究中的药物相似性方面表现出良好的结合亲和力。总体而言,是一种具有生物活性的植物,可能是药物先导物的潜在来源,值得进一步深入研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f39a/7587548/2ef0f4688287/molecules-25-04737-g001.jpg

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