Kenchappa Pratap G, Karthik Yalpi, Vijendra Poornima D, Hallur Raghavendra L S, Khandagale Ajay S, Pandurangan Ashok K, Jayanna Sathisha G, Alshehri Mohammed Ali, Alasmari Abdulrahman, Sayed Samy, Shantaram Manjula, Mushtaq Muntazir
Department of Studies and Research in Biochemistry, Jnana Kaveri Post Graduate Centre, Mangalore University, Kodagu, Karnataka, India.
Department of Studies and Research in Microbiology, Jnana Kaveri Campus, Mangalore University, Kodagu, Karnataka, India.
Front Pharmacol. 2023 May 10;14:1139606. doi: 10.3389/fphar.2023.1139606. eCollection 2023.
Alzheimer's disease (AD) is a type of neurodegenerative disease, associated with the hastening of ROS, acetylcholinesterase (AChE) activity, and amyloid β peptides plaques in the brain. The limitations and side effects of existing synthetic drugs incline toward natural sources. In the present communication active principles of methanolic extract of Roxb, leaves are explored as an antioxidant, AChE inhibitor, and anti-amyloidogenic. Furthermore, neuroprotection against the amyloid beta-peptide has been studied. The bioactive principles were identified by GC-MS and LC-MS and further subjected to antioxidant (DPPH and FRAP) and neuroprotection (AChE inhibition, ThT binding, and MTT assay, DCFH-DA and lipid peroxidation (LPO) assay using neuroblastoma (SHSY-5Y) cell lines) assays. Methanolic extract of Roxb, leaves was found to contain polyphenols and flavonoids. assays exhibited potential antioxidant and anti-AChE (˃50%) activities. ThT binding assay indicated protection against amyloid-beta aggregation. MTT assay, Aβ1-40 (10 µM) with extract increase the cell viability (˃50%) and showed significant cytotoxicity to SHSY-5Y cells. ROS level (˃25%) significantly decreased in the Aβ1-40 (10 µM) + extract (15 and 20 μM/mL) and LPO assay (˃50%) suggesting prevention of cell damage. Results advocate that leaves are a good source of antioxidants, anti-AChE, and anti-amyloidogenic compounds which may be further evaluated as a natural medicine for the treatment of AD.
阿尔茨海默病（AD）是一种神经退行性疾病，与大脑中活性氧（ROS）的加速产生、乙酰胆碱酯酶（AChE）活性以及淀粉样β肽斑块有关。现有合成药物的局限性和副作用促使人们倾向于寻找天然来源。在本通讯中，对萝芙木（Roxb）叶甲醇提取物的活性成分进行了研究，探讨其作为抗氧化剂、AChE抑制剂和抗淀粉样蛋白生成剂的作用。此外，还研究了其对淀粉样β肽的神经保护作用。通过气相色谱-质谱联用（GC-MS）和液相色谱-质谱联用（LC-MS）鉴定了生物活性成分，并进一步进行了抗氧化（二苯基苦味酰基自由基（DPPH）和铁离子还原抗氧化能力（FRAP））和神经保护（AChE抑制、硫代黄素T（ThT）结合以及使用神经母细胞瘤（SHSY-5Y）细胞系进行的MTT法、2',7'-二氯二氢荧光素二乙酸酯（DCFH-DA）和脂质过氧化（LPO）测定）测定。发现萝芙木叶甲醇提取物含有多酚和黄酮类化合物。测定显示其具有潜在的抗氧化和抗AChE（>50%）活性。ThT结合测定表明其对淀粉样β聚集具有保护作用。MTT测定表明，Aβ1-40（10 μM）与提取物共同作用可提高细胞活力（>50%），且对SHSY-5Y细胞显示出显著的细胞毒性。在Aβ1-40（10 μM）+提取物（15和20 μM/mL）中，ROS水平显著降低（>25%），LPO测定结果（>50%）表明可预防细胞损伤防止细胞损伤。结果表明，萝芙木叶是抗氧化剂、抗AChE和抗淀粉样蛋白生成化合物的良好来源，可进一步评估其作为治疗AD的天然药物的潜力。
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