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紫堇生物碱的胆碱酯酶抑制及抗遗忘活性

Cholinesterase inhibitory and anti-amnesic activity of alkaloids from Corydalis turtschaninovii.

作者信息

Hung Tran Manh, Na Minkyun, Dat Nguyen Tien, Ngoc Tran Minh, Youn Uijoung, Kim Hong Jin, Min Byung-Sun, Lee Jongpill, Bae Kihwan

机构信息

College of Pharmacy, Chungnam National University, Daejeon 305-764, Republic of Korea.

出版信息

J Ethnopharmacol. 2008 Sep 2;119(1):74-80. doi: 10.1016/j.jep.2008.05.041. Epub 2008 Jun 13.

DOI:10.1016/j.jep.2008.05.041
PMID:18601993
Abstract

In the course of screening plants used in Korean folk medicine as memory enhancers, a 70% ethanol extract of tuber from Corydalis turtschaninovii Besser (Papaveraceae) showed significant acetylcholinesterase (AChE) inhibitory activity. Repeated column chromatography led to the isolation of a new aporphine alkaloid, oxoglaucidaline (9), and a new protoberberine, pseudodehydrocorydaline (13) together with 14 known compounds (1-8, 10-12, and 14-16). The chemical structures of isolated compounds were elucidated base on extensive 1D and 2D NMR spectroscopic data. Compounds 1-16 were investigated in vitro for their anti-cholinesterase activity using the mice cortex AChE enzyme. In further study, the anti-amnesic activities of pseudoberberine (16) in mice on the learning and memory impairments induced by scopolamine (1.0 mg/kg, i.p.) were examined. This alkaloid (5.0 mg/kg, p.o.) administration significantly reversed cognitive impairments in mice by passive avoidance test (P<0.05). It also reduced escape latencies in training trials and prolonged swimming times in the target quadrant during the probe trial in the water maze task (P<0.05). These results indicated that Corydalis turtschaninovii due to its alkaloids have anti-cholinesterase activity and pseudoberberine and other alkaloids have anti-amnesic activities that may be useful for cognitive impairment treatment.

摘要

在筛选韩国民间医学中用作记忆增强剂的植物过程中,延胡索(罂粟科)块茎的70%乙醇提取物显示出显著的乙酰胆碱酯酶(AChE)抑制活性。通过反复柱色谱法分离得到一种新的阿朴啡生物碱,氧代紫堇灵(9)和一种新的原小檗碱,伪脱氢紫堇碱(13)以及14种已知化合物(1-8、10-12和14-16)。基于广泛的一维和二维核磁共振光谱数据阐明了分离化合物的化学结构。使用小鼠皮质AChE酶对化合物1-16进行了体外抗胆碱酯酶活性研究。在进一步的研究中,检测了伪小檗碱(16)对东莨菪碱(1.0 mg/kg,腹腔注射)诱导的小鼠学习和记忆障碍的抗遗忘活性。该生物碱(5.0 mg/kg,口服)给药通过被动回避试验显著逆转了小鼠的认知障碍(P<0.05)。在水迷宫任务的探测试验中,它还缩短了训练试验中的逃避潜伏期,并延长了目标象限中的游泳时间(P<0.05)。这些结果表明,延胡索因其生物碱具有抗胆碱酯酶活性,伪小檗碱和其他生物碱具有抗遗忘活性,可能对认知障碍治疗有用。

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