Department of Clinical Analysis, College of Pharmacy, Hawler Medical University, Erbil, Iraq.
Department of Pharmaceutical Chemistry, College of Pharmacy, Hawler Medical University, Erbil, Iraq.
PLoS One. 2023 Jan 25;18(1):e0280464. doi: 10.1371/journal.pone.0280464. eCollection 2023.
Methanolic extract from Onopordum acanthium L. leaves (MEOAL) has been discovered to treat diabetic complications. The objective of this study is to evaluate the ameliorative role of MEOAL on pancreatic islet injury and myocardial inflammation in diabetic rats.
Forty male Wister albino rats were allocated into five groups of eight rats each. Group A was the negative control group. Single intraperitoneal injection of streptozocin (50mg/kg) were used for the four experimental groups. Group B served as the positive control group. The rats in Groups C, D, and E received glibenclamide (5mg/kg), MEOAL (200, and 400 mg/kg) respectively, for eight weeks. Group C served as the standard drug group. High performance liquid chromatography (HPLC) and 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH) assays for antioxidant activity were conducted in MEOAL. In silico study, calculation of molecular binding energy (DG), and inhibition constant (pKi) of bioactive constituents in MEOAL were performed.
Administration of MEOAL significantly increases insulin content in β-cells with a marked enhancement of pancreatic islet structure, resulting in a significant reduction of blood glucose level and body weight loss. MEOAL treatment suppressed the increase of inflammatory cell score in myocardial tissue with an elevation of M2 -like macrophage. The phytochemical studies recorded the presence of six polyphenols, including catechin, kaempferol, syringic acid, p-coumaric acid, epicatechin and gallic acid in MEOAL. Moreover, the antioxidant activity of the extract was greater than that of standard ascorbic acid. The docking studies of the ligands Catechin, kaempferol and epicatechin with proteins showed high affinities with various targets related in β-Cells and cardiac inflammation.
The attenuation of pancreatic β-Cells damage and cardiac inflammation by MEOAL could be attributed to the presence of Catechin, kaempferol and epicatechin which have high affinities with the receptors namely pancreatic alpha-amylase, glucokinase, COX-2, and COX-1.
从牛蒡属植物叶中提取的甲醇提取物（MEOAL）已被发现可用于治疗糖尿病并发症。本研究旨在评估 MEOAL 对糖尿病大鼠胰岛损伤和心肌炎症的改善作用。
将 40 只雄性 Wister 白化大鼠分为 5 组，每组 8 只。第 A 组为阴性对照组。对 4 组实验大鼠进行单次腹腔注射链脲佐菌素（50mg/kg）。第 B 组为阳性对照组。第 C、D 和 E 组大鼠分别给予格列本脲（5mg/kg）、MEOAL（200 和 400mg/kg），连续 8 周。第 C 组为标准药物组。采用高效液相色谱（HPLC）和 2,2-二苯基-1-苦基肼水合物（DPPH）法测定 MEOAL 的抗氧化活性。采用计算机模拟方法，计算 MEOAL 中生物活性成分的分子结合能（DG）和抑制常数（pKi）。
MEOAL 给药可显著增加 β 细胞中的胰岛素含量，显著改善胰岛结构，显著降低血糖水平和体重减轻。MEOAL 治疗可抑制心肌组织中炎症细胞评分的升高，并增加 M2 样巨噬细胞。植物化学研究记录了 MEOAL 中存在的 6 种多酚，包括儿茶素、山奈酚、丁香酸、对香豆酸、表儿茶素和没食子酸。此外，提取物的抗氧化活性强于标准抗坏血酸。配体儿茶素、山奈酚和表儿茶素与蛋白质的对接研究表明，它们与与β细胞和心脏炎症相关的各种靶标具有高亲和力。
MEOAL 减轻胰岛β细胞损伤和心脏炎症的作用可能归因于儿茶素、山奈酚和表儿茶素的存在，它们与胰腺α-淀粉酶、葡萄糖激酶、COX-2 和 COX-1 等受体具有高亲和力。
