Kim Cho Rong, Choi Soo Jung, Kwon Yoon Kyung, Kim Jae Kyeom, Kim Youn-Jung, Park Gwi Gun, Shin Dong-Hoon
Department of Food and Biotechnology, Korea University.
Biol Pharm Bull. 2016;39(7):1130-6. doi: 10.1248/bpb.b16-00045.
The pathogenesis of Alzheimer's disease (AD) has been linked to the deficiency of neurotransmitter acetylcholine (ACh) in the brain, and the main treatment strategy for improving AD symptoms is the inhibition of acetylcholinesterase (AChE) activity. In the present study, we aimed to identify potent AChE inhibitors from Cinnamomum loureirii extract via bioassay-guided fractionation. We demonstrated that the most potent AChE inhibitor present in the C. loureirii extract was 2,4-bis(1,1-dimethylethyl)phenol. To confirm the antiamnesic effects of the ethanol extract of C. loureirii, mice were intraperitoneally injected with the neurotoxin trimethyltin (2.5 mg/kg) to induce cognitive dysfunction, and performance in the Y-maze and passive avoidance tests was assessed. Treatment with C. loureirii extract significantly improved performance in both behavioral tests, suggesting that this extract may be neuroprotective and therefore beneficial in preventing or ameliorating the degenerative processes of AD, potentially by restoring cholinergic function.
阿尔茨海默病（AD）的发病机制与大脑中神经递质乙酰胆碱（ACh）的缺乏有关，改善AD症状的主要治疗策略是抑制乙酰胆碱酯酶（AChE）的活性。在本研究中，我们旨在通过生物测定引导的分级分离从阴香提取物中鉴定出有效的AChE抑制剂。我们证明阴香提取物中最有效的AChE抑制剂是2,4-双（1,1-二甲基乙基）苯酚。为了证实阴香乙醇提取物的抗记忆作用，给小鼠腹腔注射神经毒素三甲基锡（2.5mg/kg）以诱导认知功能障碍，并评估其在Y迷宫和被动回避试验中的表现。阴香提取物治疗显著改善了两项行为测试中的表现，表明该提取物可能具有神经保护作用，因此可能通过恢复胆碱能功能对预防或改善AD的退行性过程有益。
