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[具体物质名称]通过阻断大麻素受体对高脂饮食诱导肥胖大鼠的抗肥胖作用

Anti-Obesity Action of in Rats against High-Fat Diet-Induced Obesity by Blocking the Cannabinoid Receptors.

作者信息

Khalid Mohammad, Alqarni Mohammed H, Shoaib Ambreen, Wahab Shadma, Foudah Ahmed I, Aljarba Tariq M, Akhtar Juber, Alamri Mubarak A, Ahmad Sarfaraz

机构信息

Department of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi Arabia.

Department of Clinical Pharmacy, College of Pharmacy, Jazan University, P.O. Box 114, Jazan 45142, Saudi Arabia.

出版信息

Plants (Basel). 2022 Apr 25;11(9):1158. doi: 10.3390/plants11091158.

Abstract

Obesity, type 2 diabetes, and cardiovascular illnesses have known risk factors in the pathophysiology of an unhealthy diet. Obesity now affects almost a third of the world's population and is widely seen as a side effect of the Industrial Revolution. The current study aimed to determine natural phytoconstituents that have a significant role in the management of obesity. In this view, we have selected the plant which has different pharmacological actions and is traditionally used to treat sickness caused by lifestyle modification. The methanolic extract of the plant material was prepared and then further fractionated by means of solvents (n-hexane, chloroform, n-butanol, and water). The absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis was done by taking the active constituent of the plant (Punarnavine, Boeravinone B, and Eupalitin). The molecular docking analysis of these compounds is also performed by targeting the cannabinoid receptor (CR). Structural analysis of the best complex was done using the Discovery Studio visualizer tool. High-performance thin-layer chromatography (HPTLC) analysis was done by using a solvent system (chloroform and methanol in a ratio of 8:2). The study was done on the Sprague-Dawley (SD) rats treated with a high-fat diet to induce obesity and different parameters such as body weight, behavioral activity, organ fat pad weight, lipid profile, and liver biomarkers (AST, ALT, BUN, and creatinine) were estimated. The result of the study suggested that the phytoconstituents of upon molecular docking revealed the possible binding mechanisms with the CR and thus show potent anti-obesity action.

摘要

肥胖、2型糖尿病和心血管疾病在不健康饮食的病理生理学中存在已知的风险因素。肥胖目前影响着全球近三分之一的人口,被广泛视为工业革命的副作用。当前的研究旨在确定在肥胖管理中起重要作用的天然植物成分。基于此观点,我们选择了一种具有不同药理作用且传统上用于治疗因生活方式改变引起疾病的植物。制备了该植物材料的甲醇提取物,然后通过溶剂(正己烷、氯仿、正丁醇和水)进一步分离。通过采用该植物的活性成分(刺蒺藜苷、波热拉黄酮B和优帕利亭)进行吸收、分布、代谢、排泄和毒性(ADMET)分析。还通过靶向大麻素受体(CR)对这些化合物进行分子对接分析。使用Discovery Studio可视化工具对最佳复合物进行结构分析。通过使用氯仿和甲醇比例为8:2的溶剂系统进行高效薄层色谱(HPTLC)分析。对用高脂饮食诱导肥胖的斯普拉格-道利(SD)大鼠进行了研究,并评估了体重、行为活动、器官脂肪垫重量、血脂谱和肝脏生物标志物(AST、ALT、BUN和肌酐)等不同参数。研究结果表明,该植物的植物成分经分子对接揭示了与CR的可能结合机制,从而显示出有效的抗肥胖作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1d6/9105516/0da545590e3e/plants-11-01158-g001.jpg

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