Department of Medicinal Chemistry, School of Pharmacy, Medicinal Plants and Natural Products Research Center, Hamadan University of Medical Sciences, Hamadan, Iran.
Department of Pharmacognosy, School of Pharmacy, Medicinal Plants and Natural Products Research Center, Hamadan University of Medical Sciences, Hamadan, Iran.
J Biomol Struct Dyn. 2021 Jun;39(9):3235-3243. doi: 10.1080/07391102.2020.1764391. Epub 2020 May 15.
Alzheimer's disease is a progressive neurodegenerative disorder and patients suffer from memory loss, a decline in language skill and impairment in other cognitive functions. In the cholinergic hypothesis, dysfunction of cholinergic neurons especially in the hippocampus and cerebral cortex contributes to cognitive decline in patients. So agents that enhance acetylcholine concentration could improve cognitive function. AChEIs are among the most studied anti-Alzheimer agents. Galbanic acid as a natural compound with a sesquiterpene coumarin scaffold is a weak inhibitor of AChE. In the present contribution, we discussed the impact of carboxylic group ionization on inhibitory effects. We performed and studies on galbanic acid, methyl and ethyl galbanates as AChE inhibitors. The order of inhibitory effect on AChE was obtained as ethyl galbanate ∼ methyl galbanate > galbanic acid. Our study highlights the important role of the physicochemical properties of natural lead compounds in each specific assay.Communicated by Ramaswamy H. Sarma.
阿尔茨海默病是一种进行性神经退行性疾病，患者会出现记忆丧失、语言技能下降和其他认知功能障碍。在胆碱能假说中，胆碱能神经元功能障碍，特别是海马体和大脑皮层的胆碱能神经元功能障碍，导致患者认知能力下降。因此，能提高乙酰胆碱浓度的药物可以改善认知功能。乙酰胆碱酯酶抑制剂是研究最多的抗阿尔茨海默病药物之一。贺斯卡酸作为一种具有倍半萜香豆素骨架的天然化合物，是一种弱乙酰胆碱酯酶抑制剂。在本研究中，我们讨论了羧酸基团离解对抑制作用的影响。我们对贺斯卡酸、甲基贺斯卡酸和乙基贺斯卡酸作为乙酰胆碱酯酶抑制剂进行了 和 研究。对乙酰胆碱酯酶的抑制作用顺序为乙基贺斯卡酸≈甲基贺斯卡酸>贺斯卡酸。我们的研究强调了天然先导化合物在每个特定测定中的物理化学性质的重要作用。由 Ramaswamy H. Sarma 传达。
