目的:从山莨菪根部的总生物碱提取物中分离乙酰胆碱酯酶抑制剂。方法:山莨菪根经95%乙醇提取、4mol/LHCl和4mol/LNaOH酸碱处理,氯仿萃取,得到总生物碱。采用薄层色谱生物自显影法跟踪分离目标组分,再用改良的Ellman法进一步测定抑制率。利用多种柱色谱分离得到3个化合物(1-3),通过^1 H-NMR、^13 C-NMR、ESI-MS波谱方法并与文献比对鉴定化合物的结构。结果:从山莨菪根部的总生物碱提取物中分离得到3个已知化合物,它们分别被鉴定为东莨菪碱,樟柳碱,阿托品,其乙酰胆碱酯酶抑制率分别为45.28%,38.08%和25.10%。结论:莨菪碱衍生物具有较弱的乙酰胆碱酯酶抑制活性。
Objective : To isolate acetylcholinesterase inhibitor from total alkaloidal extracted of the roots of Anisodus tan- guteus. Method : The root of Anisodus tangutcus were extracted by 95 % ethanol and treated with 4 mol · L^-1HCl and 4 mol · L^-1 NaOH , and then extracted by chloroform to obtain total alkaloidal extracts. The bioassay -guided isolation of the AChE inhibitor was executed by TLC bioautographic method , and modified Ellman' s colorimetric method in 96 - well microplates. Three compounds ( 1 - 3 ) were obtainded by various column chromatographic methods and their struc- tures were elucidated based on1HNMR, 13 C - NMR , ESI - MS analysis and compared with literature reports. Result : Three known compounds were isolated and identified as scopolamine, anisodine, atropine, respectively. Their inhibitory rates of 1 -3 against AchE were 45.28%, 38.08% and 25.10%, respectively. Conclusion: Derivatives of hyoseyamine have a weak inhibitory activity to AchE.