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采用分子动力学模拟评估从酸橙皮中分离的柠檬苦素的体外抗糖尿病活性。

Assessment of the in vitro anti-diabetic activity with molecular dynamic simulations of limonoids isolated from Adalia lemon peels.

机构信息

Pharmacognosy Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre, 33 El Bohouth St. (Former El Tahrir St.), P.O. 12622, Dokki, Giza, Egypt.

Biochemistry Department, Biotechnology Research Institute, National Research Centre, 33 El Bohouth St. (Former El Tahrir St.), P.O. 12622, Dokki, Giza, Egypt.

出版信息

Sci Rep. 2024 Sep 14;14(1):21478. doi: 10.1038/s41598-024-71198-5.

Abstract

Limonoids are important constituents of citrus that have a significant impact on promoting human health. Therefore, the primary focus of this research was to assess the overall limonoid content and isolate limonoids from Adalia lemon (Citrus limon L.) peels for their potential use as antioxidants and anti-diabetic agents. The levels of limonoid aglycones in the C. limon peel extract were quantified through a colorimetric assay, revealing a concentration of 16.53 ± 0.93 mg/L limonin equivalent. Furthermore, the total concentration of limonoid glucosides was determined to be 54.38 ± 1.02 mg/L. The study successfully identified five isolated limonoids, namely limonin, deacetylnomilin, nomilin, obacunone 17-O-β-D-glucopyranoside, and limonin 17-O-β-D-glucopyranoside, along with their respective yields. The efficacy of the limonoids-rich extract and the five isolated compounds was evaluated at three different concentrations (50, 100, and 200 µg/mL). It was found that both obacunone 17-O-β-D-glucopyranoside and limonin 17-O-β-D-glucopyranoside possessed the highest antioxidant, free radical scavenging, and anti-diabetic activities, followed by deacetylnomilin, and then the limonoids-rich extract. The molecular dynamic simulations were conducted to predict the behavior of the isolated compounds upon binding to the protein's active site, as well as their interaction and stability. The results revealed that limonin 17-O-β-D-glucopyranoside bound to the protein complex system exhibited a relatively more stable conformation than the Apo system. The analysis of Solvent Accessible Surface Area (SASA), in conjunction with the data obtained from Root-Mean-Square Deviation (RMSD), Root-Mean-Square Fluctuation (RMSF), and Radius of Gyration (ROG) computations, provided further evidence that the limonin 17-O-β-D-glucopyranoside complex system remained stable within the catalytic domain binding site of the human pancreatic alpha-amylase (HPA)-receptor. The research findings suggest that the limonoids found in Adalia lemon peels have the potential to be used as effective natural substances in creating innovative therapeutic treatments for conditions related to oxidative stress and disorders in carbohydrate metabolism.

摘要

类柠檬苦素是柑橘中的重要成分,对促进人体健康有重要影响。因此,本研究的主要重点是评估从 Adalia 柠檬(Citrus limon L.)果皮中提取的类柠檬苦素的总含量,并分离类柠檬苦素,以将其用作抗氧化剂和抗糖尿病药物。通过比色法测定 C. limon 皮提取物中类柠檬苦素配糖体的水平,发现柠碱当量浓度为 16.53 ± 0.93 mg/L。此外,类柠檬苦素糖苷的总浓度确定为 54.38 ± 1.02 mg/L。该研究成功鉴定了五种分离的类柠檬苦素,分别为柠碱、去乙酰诺米林、诺米林、obacunone 17-O-β-D-吡喃葡萄糖苷和柠碱 17-O-β-D-吡喃葡萄糖苷,以及它们各自的产率。在三个不同浓度(50、100 和 200 μg/mL)下评估了富含类柠檬苦素的提取物和五种分离化合物的功效。结果发现,obacunone 17-O-β-D-吡喃葡萄糖苷和 limonin 17-O-β-D-吡喃葡萄糖苷具有最高的抗氧化、自由基清除和抗糖尿病活性,其次是去乙酰诺米林,然后是富含类柠檬苦素的提取物。进行分子动力学模拟以预测分离化合物与蛋白质活性位点结合时的行为,以及它们的相互作用和稳定性。结果表明,与 Apo 系统相比,柠碱 17-O-β-D-吡喃葡萄糖苷与蛋白质复合系统结合时表现出相对更稳定的构象。溶剂可及表面积(SASA)的分析,结合根均方偏差(RMSD)、根均方波动(RMSF)和回转半径(ROG)计算的数据,进一步证明了柠碱 17-O-β-D-吡喃葡萄糖苷复合物系统在人胰腺α-淀粉酶(HPA)-受体的催化域结合位点保持稳定。研究结果表明,Adalia 柠檬皮中的类柠檬苦素有潜力作为有效的天然物质,用于开发与氧化应激和碳水化合物代谢紊乱相关的创新治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/14b1/11401861/309a38247ed3/41598_2024_71198_Fig1_HTML.jpg

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