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
Selcuk University, Science Faculty, Department of Biology, Campus, 42250, Konya, Turkey.
Department of Medicinal Laboratory, Vocational School of Health Services, Selcuk University, Konya, Turkey.
Biomed Pharmacother. 2017 Mar;87:27-36. doi: 10.1016/j.biopha.2016.12.063. Epub 2016 Dec 29.
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.
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。
