植物来源的生物碱类乙酰胆碱酯酶抑制剂研究进展

乙酰胆碱酯酶抑制剂是阿尔茨海默病治疗药物的研究热点。根据类胆碱学说,乙酰胆碱酯酶抑制剂可提高脑部神经递质乙酰胆碱的水平从而改善阿尔茨海默病患者的胆碱功能,并缓解神经性紊乱的症状。植物天然产物是乙酰胆碱酯酶抑制剂先导化合物的重要来源,其中生物碱为此类天然产物的重要组成部分。综述植物来源且具有抗乙酰胆碱酯酶活性生物碱的结构类型、作用机制及其构效关系。

Research progress on plant-derived acetylcholinesterase inhibitory alkaloids

Acetylcholinesterase (AChE) inhibitor is a research hotspot in the treatment of Alzheimer's disease (AD). According to the cholinergic hypothesis, the AChE inhibitors can increase the level of neurotransmitter acetylcholine in the brain, thus improving cholinergic functions in patients with AD and alleviating the symptoms of this neurological disorder. As AChE inhibitor is an important therapeutic strategy for AD, efforts are being made in the search for new molecules with anti-AChE activity. The fact that naturally-occurring compounds from plants are considered to be a potential source of new inhibitors has led to the discovery of an important number of AChE inhibitory alkaloids. Since the approval of galantamine for the treatment of AD patients, the search for new anticholinesterase alkaloids has escalated. This review summarizes recent advances in current knowledge on alkaloids as AChE inhibitors, and outlines the structure-activity relationship and docking studies.