Lam Linh My Thi, Nguyen Mai Thanh Thi, Nguyen Hai Xuan, Dang Phu Hoang, Nguyen Nhan Trung, Tran Hung Manh, Nguyen Hoa Thi, Nguyen Nui Minh, Min Byung Sun, Kim Jeong Ah, Choi Jae Sue, Van Can Mao
Faculty of Chemistry, University of Science, Vietnam National University-Hochiminh City, 227 Nguyen Van Cu, District 5, Hochiminh City, Vietnam.
Faculty of Chemistry, University of Science, Vietnam National University-Hochiminh City, 227 Nguyen Van Cu, District 5, Hochiminh City, Vietnam ; Cancer Research Laboratory, Vietnam National University-Hochiminh City, Hochiminh City, Vietnam.
Chem Cent J. 2016 Aug 3;10:48. doi: 10.1186/s13065-016-0197-5. eCollection 2016.
Alzheimer's disease (AD) is the most common cause of dementia among the elderly and is characterized by loss of memory and other cognitive functions. An increase in AChE (a key enzyme in the cholinergic nervous system) levels around β-amyloid plaques and neurofibrillary tangles is a common feature of AD neuropathology. Amnesic effects of scopolamine (acetylcholine receptor antagonist) can be investigated in various behavioral tests such as Morris water maze, object recognition, Y-maze, and passive avoidance. In the scope of this paper, we report the anti-AChE, anti-BChE properties of the isolated compound and the in vivo effects of the methanolic extract of Xylia xylocarpa (MEXX) on scopolamine-induced memory deficit.
In further phytochemistry study, a new hopan-type triterpenoid, (3β)-hopan-3-ol-28,22-olide (1), together with twenty known compounds were isolated (2-21). Compound 1, 2, 4, 5, 7-9, and 11-13 exhibited potent acetylcholinesterase (AChE) inhibitory activity in a concentration-dependent manner with IC50 values ranging from 54.4 to 94.6 μM. Compound 13 was also shown anti-butyrylcholinesterase (BChE) activity with an IC50 value of 42.7 μM. The Morris water Y-maze, Y-maze, and object recognition test were also carried out.
It is noteworthy that MEXX is effective when administered orally to mice, experimental results are consistent with the traditional use of this medicinal plant species.
阿尔茨海默病(AD)是老年人痴呆最常见的病因,其特征为记忆及其他认知功能丧失。β-淀粉样斑块和神经原纤维缠结周围乙酰胆碱酯酶(胆碱能神经系统中的一种关键酶)水平升高是AD神经病理学的一个常见特征。东莨菪碱(乙酰胆碱受体拮抗剂)的失忆效应可在多种行为测试中进行研究,如莫里斯水迷宫、物体识别、Y迷宫和被动回避测试。在本文范围内,我们报道了分离得到的化合物的抗乙酰胆碱酯酶、抗丁酰胆碱酯酶特性以及木荚豆甲醇提取物(MEXX)对东莨菪碱诱导的记忆缺陷的体内作用。
在进一步的植物化学研究中,分离得到一种新的何帕烷型三萜,(3β)-何帕-3-醇-28,22-内酯(1),以及20种已知化合物(2-21)。化合物1、2、4、5、7-9和11-13以浓度依赖的方式表现出强大的乙酰胆碱酯酶(AChE)抑制活性,IC50值范围为54.4至94.6μM。化合物13也表现出抗丁酰胆碱酯酶(BChE)活性,IC50值为42.7μM。还进行了莫里斯水Y迷宫、Y迷宫和物体识别测试。
值得注意的是,MEXX口服给药对小鼠有效,实验结果与该药用植物的传统用途一致。