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首页> 外文期刊>Natural product communications >Acetylcholinesterase and butyrylcholinesterase inhibitory compounds from Corydalis cava (Fumariaceae)
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Acetylcholinesterase and butyrylcholinesterase inhibitory compounds from Corydalis cava (Fumariaceae)

机译:延胡索中的乙酰胆碱酯酶和丁酰胆碱酯酶抑制化合物

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摘要

Tubers of Corydalis cava were extracted with ethanol and fractionated using n-hexane, chloroform and ethanol. Repeated column chromatography, preparative TLC and crystallization led to the isolation of fifteen isoquinoline alkaloids. The chemical structures of the isolated compounds were determined on the basis of spectroscopic techniques and by comparison with literature data. All isolated compounds were tested for human blood acetylcholinesterase (HuAChE) and human plasma butyrylcholinesterase (HuBuChE) inhibitory activity. (+)-Canadaline inhibited acetylcholinesterase as well as butyrylcholinesterase in a dose-dependent manner with IC_(50) values of 20.1 ± 1.1 μM and 85.2 ± 3.2 μM, respectively. (+)-Canadine, with an IC_(50) value of 12.4 ± 0.9 μM, was the most potent inhibitor of acetylcholinesterase, whilst (±)-corycavidine and (+)-bulbocapnine were effective inhibitors of butyrylcholinesterase with IC_(50) values of 46.2 ± 2.4 μM and 67.0 ± 2.1 μM, respectively. The other isolated alkaloids were considered inactive (IC_(50) > 100 μM).
机译:用乙醇提取延胡索的块茎,并用正己烷,氯仿和乙醇分级分离。重复柱层析,制备型TLC和结晶导致分离出15种异喹啉生物碱。分离的化合物的化学结构是在光谱技术的基础上确定的,并与文献数据进行了比较。测试所有分离的化合物的人血乙酰胆碱酯酶(HuAChE)和人血浆丁酰胆碱酯酶(HuBuChE)抑制活性。 (+)-加拿大碱以剂量依赖性方式抑制乙酰胆碱酯酶和丁酰胆碱酯酶,IC_(50)值分别为20.1±1.1μM和85.2±3.2μM。 (+)-Canadine的IC_(50)值为12.4±0.9μM,是最有效的乙酰胆碱酯酶抑制剂,而(±)-椰油酰胺和(+)-bulbocapnine是丁酰胆碱酯酶的有效抑制剂,IC_(50)值分别为46.2±2.4μM和67.0±2.1μM。其他分离的生物碱被认为是无活性的(IC_(50)> 100μM)。

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