Kamli Majid Rasool, Sharaf Abeer Abdullah M, Sabir Jamal S M, Rather Irfan A
Department of Biological Sciences, Faculty of Science, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Center of Excellence in Bionanoscience Research, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Plants (Basel). 2022 Feb 14;11(4):514. doi: 10.3390/plants11040514.
The inhibition of acetylcholinesterase (AChE) by cholinergic agents has been promoted as a potent strategy for treating and managing cognitive decline disorders. A wide range of natural products has long been used as potential sources or formulations of cholinergic inhibitors. Therefore, this study aimed to evaluate different L. () extracts for their AChE inhibitory activity using galanthamine as a standard AChE inhibitor. In this study, the ethyl-acetate extract (at a concentration of 250 µg/mL) exhibited the greatest inhibitory effect against AChE with significant inhibition of 75%, comparable to the inhibitor galanthamine with an inhibition of 88%. Kinetic analysis revealed that the extracts could induce a mixed type of inhibition, as observed in the case of galanthamine, with the highest increased and decreased values in the ethyl acetate extract. The antioxidant potential of the three extracts tested was found to be in the order of ethyl-acetate > ethanol > aqueous, with IC values of 272 µg/mL, 387 µg/mL, and 534 µg/mL, respectively. Ethyl-acetate was found to have the highest total phenolic content in all extracts. Further, in silico study showed structural binding characterization of rosmarinic acid and carnosic acid with human AChE enzyme. Rosmarinic acid showed strong binding and formed two hydrogen-bonding interactions with Ser-293 and Arg-296. In light of this, the ethyl-acetate extract of the plant may provide some novel potential pharmacological leads for treating and managing cognitive disorders such as Alzheimer's.
胆碱能药物对乙酰胆碱酯酶(AChE)的抑制作用已被视为治疗和管理认知功能衰退障碍的有效策略。长期以来,多种天然产物一直被用作胆碱能抑制剂的潜在来源或制剂。因此,本研究旨在以加兰他敏作为标准AChE抑制剂,评估不同的迷迭香叶提取物的AChE抑制活性。在本研究中,乙酸乙酯提取物(浓度为250μg/mL)对AChE表现出最大的抑制作用,显著抑制率为75%,与抑制率为88%的抑制剂加兰他敏相当。动力学分析表明,提取物可诱导混合型抑制,如加兰他敏的情况,乙酸乙酯提取物的最大增加和减少值最高。所测试的三种提取物的抗氧化潜力顺序为乙酸乙酯>乙醇>水,IC值分别为272μg/mL、387μg/mL和534μg/mL。发现乙酸乙酯在所有提取物中的总酚含量最高。此外,计算机模拟研究显示了迷迭香酸和肌醇六磷酸与人类AChE酶的结构结合特征。迷迭香酸显示出强结合,并与Ser-293和Arg-296形成两个氢键相互作用。有鉴于此,该植物的乙酸乙酯提取物可能为治疗和管理如阿尔茨海默病等认知障碍提供一些新的潜在药理学线索。