Karpuz Ağören Büşra, Küpeli Akkol Esra, Çelik Ismail, Sobarzo-Sánchez Eduardo
Department of Pharmacognosy, Faculty of Pharmacy, Başkent University, Ankara, Türkiye.
Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, Ankara, Türkiye.
Front Pharmacol. 2024 Aug 28;15:1443173. doi: 10.3389/fphar.2024.1443173. eCollection 2024.
The World Health Organization reports that 30% of adults worldwide suffer from insomnia, while 10% of people worldwide suffer with various forms of anxiety. The significant negative effects of conventional medications used to treat anxiety and insomnia, such as abuse, addiction, amnesia, and cognitive and sexual dysfunction, have led to an increased preference for naturally derived substances with fewer side effects. Accordingly, in this study, the sedative and anxiolytic effects of -hexane, ethyl acetate (EtOAc), methanol (MeOH) and water extracts of the aerial parts of Duhamel., which is used for sedative purposes in folk medicine, were evaluated. To evaluate the sedative and anxiolytic effects of each extract, bioassay systems were used including traction and hole-board tests. The MeOH extract of was the most active extract on traction and hole-board tests compared to Diazepam. From the MeOH extract, major components were isolated, and their structures were identified as three flavonoid glycosides [rutin (1), quercetin-3--glucoside (2), and quercetin 3--rhamnoside (3)] using spectral techniques. The most abundant component was determined to be rutin, comprising 8 mg/100 mg dry extract in MeOH extract and 76.7 mg/100 mg dry fraction in fraction C using HPLC. The molecular docking studies evaluated the interaction of isolated flavonoid glycosides with the interaction energies and protein-ligand interaction details of the anxiety-related receptors GABAA and GABAB. For the GABAA receptor, quercetin-3--glucoside demonstrated the highest docking score. Quercetin-3--rhamnoside and rutin also show promising interactions, particularly with the GABAB receptor, highlighting their potential as modulators of these receptors. In conclusion, the use of for sedative purposes in folk medicine has been confirmed for the first time by studies, and its possible active compounds and sedative-anxiolytic mechanism have been determined through phytochemical and studies.
世界卫生组织报告称，全球30%的成年人患有失眠症，而全球10%的人患有各种形式的焦虑症。用于治疗焦虑症和失眠症的传统药物具有显著的负面影响，如滥用、成瘾、失忆以及认知和性功能障碍，这使得人们越来越倾向于选择副作用较少的天然衍生物质。因此，在本研究中，对民间医学中用于镇静目的的杜氏鼠尾草地上部分的正己烷、乙酸乙酯（EtOAc）、甲醇（MeOH）和水提取物的镇静和抗焦虑作用进行了评估。为了评估每种提取物的镇静和抗焦虑作用，使用了包括牵引和洞板试验在内的生物测定系统。与地西泮相比，杜氏鼠尾草的甲醇提取物在牵引和洞板试验中是最具活性的提取物。从甲醇提取物中分离出主要成分，并使用光谱技术将其结构鉴定为三种黄酮苷[芦丁（1）、槲皮素-3-O-葡萄糖苷（2）和槲皮素3-O-鼠李糖苷（3）]。通过高效液相色谱法测定，最丰富的成分是芦丁，在甲醇提取物中为8mg/100mg干提取物，在C级分中为76.7mg/100mg干馏分。分子对接研究评估了分离出的黄酮苷与焦虑相关受体GABAA和GABAB的相互作用能量以及蛋白质-配体相互作用细节。对于GABAA受体，槲皮素-3-O-葡萄糖苷表现出最高的对接分数。槲皮素3-O-鼠李糖苷和芦丁也显示出有前景的相互作用，特别是与GABAB受体，突出了它们作为这些受体调节剂的潜力。总之，本研究首次证实了民间医学中使用杜氏鼠尾草进行镇静的用途，并通过植物化学和分子对接研究确定了其可能的活性化合物和镇静抗焦虑机制。
