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齿裂大戟:开发新型功能性制剂的有前景的植物药来源。

Euphorbia denticulata Lam.: A promising source of phyto-pharmaceuticals for the development of novel functional formulations.

作者信息

Zengin Gokhan, Uysal Ahmet, Aktumsek Abdurrahman, Mocan Andrei, Mollica Adriano, Locatelli Marcello, Custodio Luisa, Neng Nuno R, Nogueira José M F, Aumeeruddy-Elalfi Zaahira, Mahomoodally M Fawzi

机构信息

Selcuk University, Science Faculty, Department of Biology, Campus, 42250, Konya, Turkey.

Department of Medicinal Laboratory, Vocational School of Health Services, Selcuk University, Konya, Turkey.

出版信息

Biomed Pharmacother. 2017 Mar;87:27-36. doi: 10.1016/j.biopha.2016.12.063. Epub 2016 Dec 29.

Abstract

In this study, Methanolic extracts of Euphorbia denticulata parts (flowers, leaf, stem, and mix of aerial parts) were assessed for a panoply of bioactivities. Inhibitory potential against key enzymes involved in diabetes (α-glucosidase and α-amylase), obesity (pancreatic lipase), neurodegenerative diseases (cholinesterases), and hyperpigmentation (tyrosinase) was evaluated. The antioxidant and antibacterial properties were also assessed. The total phenolic, flavonoid, and phytochemical profile were established using HPLC/DAD and molecular modelling studies on specific target compounds were performed in silico. The flower extract was found to be rich in phenolics and flavonoids, (60.11±1.40mgGAE/g and 42.04±0.16mgRE/g respectively), which tend to correlate with the high radical scavenging activity of this extract (120.34±3.33mgTE/g and 165.42±2.16mgTE/g for DPPH and ABTS respectively). Catechin, epicatechin, gallic acid, p-OH-Benzoic acid, rosmarinic acid, and epigallocatechin gallate, found in significant abundance in the extracts were assessed using molecular modelling with the aim to study their docking properties on a set of six enzymes used in this study. The extracts were moderately effective with MIC values ranging between 1.56 to 6.25mg/ml, but potent growth inhibitors of MRSA strains. Results amassed herein can be used as a stimulus for further studies geared towards the development of novel phyto-pharmaceuticals.

摘要

在本研究中,对齿裂大戟各部位(花、叶、茎及地上部分混合物)的甲醇提取物进行了一系列生物活性评估。评估了其对糖尿病相关关键酶(α-葡萄糖苷酶和α-淀粉酶)、肥胖相关酶(胰脂肪酶)、神经退行性疾病相关酶(胆碱酯酶)以及色素沉着相关酶(酪氨酸酶)的抑制潜力。还评估了其抗氧化和抗菌性能。使用高效液相色谱/二极管阵列检测器(HPLC/DAD)确定了总酚、黄酮和植物化学特征,并在计算机上对特定目标化合物进行了分子模拟研究。发现花提取物富含酚类和黄酮类化合物(分别为60.11±1.40mg没食子酸当量/g和42.04±0.16mg芦丁当量/g),这与该提取物的高自由基清除活性相关(DPPH和ABTS的自由基清除活性分别为120.34±3.33mg Trolox当量/g和165.42±2.16mg Trolox当量/g)。对提取物中大量存在的儿茶素、表儿茶素、没食子酸、对羟基苯甲酸、迷迭香酸和表没食子儿茶素没食子酸酯进行了分子模拟评估,目的是研究它们在本研究中使用的六种酶上的对接特性。提取物的最低抑菌浓度(MIC)值在1.56至6.25mg/ml之间,抗菌效果中等,但对耐甲氧西林金黄色葡萄球菌(MRSA)菌株是有效的生长抑制剂。本文积累的结果可作为进一步研究开发新型植物药的推动力。

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