Adsersen Anne, Kjølbye Anne, Dall Ole, Jäger Anna K
Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, 2 Universitetsparken, Copenhagen O 2100, Denmark.
J Ethnopharmacol. 2007 Aug 15;113(1):179-82. doi: 10.1016/j.jep.2007.05.006. Epub 2007 May 6.
In the course of screening plants used in Danish folk medicine as memory enhancers, a crude methanolic extract of tubers from Corydalis cava showed significant acetylcholinesterase inhibitory activity in a dose-dependent manner. Activity guided fractionation of the methanolic extract resulted in the isolation of three alkaloids, bulbocapnine (1), corydaline (2) and corydine (3) as active constituents. Bulbocapnine inhibited acetylcholinesterase as well as butyrylcholinesterase in a dose-dependent manner with IC(50) values of 40+/-2 microM and 83+/-3 microM, respectively. Corydaline inhibited acetylcholinesterase in a dose-dependent manner with an IC(50) value of 15+/-3 microM and corydine inhibited butyrylcholinesterase in a dose-dependent manner with an IC(50) value of 52+/-4 microM. Corydaline was considered inactive against butyrylcholinesterase and corydine against acetylcholinesterase, due to IC(50)>100 microM.
在筛选丹麦民间医学中用作记忆增强剂的植物过程中，紫堇块茎的粗甲醇提取物显示出显著的乙酰胆碱酯酶抑制活性，且呈剂量依赖性。对甲醇提取物进行活性导向分级分离，得到了三种生物碱，即紫堇灵（1）、延胡索乙素（2）和紫堇定（3）作为活性成分。紫堇灵以剂量依赖性方式抑制乙酰胆碱酯酶和丁酰胆碱酯酶，IC50值分别为40±2 μM和83±3 μM。延胡索乙素以剂量依赖性方式抑制乙酰胆碱酯酶，IC50值为15±3 μM，紫堇定以剂量依赖性方式抑制丁酰胆碱酯酶，IC50值为52±4 μM。由于IC50>100 μM，延胡索乙素被认为对丁酰胆碱酯酶无活性，紫堇定对乙酰胆碱酯酶无活性。
