[关键词]
[摘要]
目的 建立从天然药物中快速发现乙酰胆碱酯酶抑制剂的有效方法,为中药及其活性成分治疗阿尔茨海默病提供支持。方法 通过Ellman比色法,对多种药用植物乙醇提取物的抗乙酰胆碱酯酶活性进行评价,筛选出活性较好的提取物样品,应用亲和超滤超高效液相色谱-四级杆-飞行时间串联质谱(UPLC-Q-TOF/MS)联用技术分离鉴定其中的活性成分。结果 元胡、黄柏、钩藤、血三七具有较强的乙酰胆碱酯酶抑制活性。经过快速筛选,发现3-二氢异卡丹宾或者3-二氢卡丹宾、钩藤碱、异钩藤碱、柯诺辛或异柯诺辛可能为钩藤中的活性化合物。结论 采用亲和超滤UPLC-Q-TOF/MS联用技术从天然药物中快速筛选出乙酰胆碱酯酶抑制剂,方法可行、快速,能够为治疗阿尔茨海默病的新药开发提供先导化合物。
[Key word]
[Abstract]
Objective To establish an effective method to rapidly detect acetylcholinesterase inhibitors from natural products, and provide support for the treatment of Alzheimer's disease with Chinese medicine and its active ingredients. Methods The activity of restraining acetylcholinesterase of crude extracts of a variety of medicinal plants were evaluated by applying Ellman's colorimetric, and the better activity of the extract sample solution was filtered out. The active ingredients of medicinal plants were identified and separated by the application of AS/UF-UPLC-MS. Results According to the experimental data, Corydais yanhusuo, Phellodendron chinense, Uncaria rhynchophylla, and Gynura segetum had significant restraining acetylcholinesterase activity. Rapid screening showed that 3α-dihydrocadambine, 3α-isodihydrocadambine, rhyncholphylline, isorhynchophylline, corynoxine, and isocorynoxine were active ingredients in U. rhynchophylla. Conclusion The results suggest that it is feasible to screen acetylcholinesterase inhibitors from natural organism plants. Using AS/UF-UPLC-MS methods, leading compounds for the development of new drugs for Alzheimer's disease would be developed and provided.
[中图分类号]
[基金项目]