具有乙酰胆碱酯酶抑制活性的总生物碱提取物的筛选

Screening of Total Alkaloidal Extracts from Plant for Acetylcholinesterase Inhibitory Activity

目的:从采自甘肃文县和舟曲的22种植物的总生物碱提取物中筛选具有乙酰胆碱酯酶抑制活性的提取物,为进一步寻找天然乙酰胆碱酯酶抑制剂单体成分奠定基础。方法:采用酸提碱沉法提取生物碱,用改良的Ellman比色法测定总生物碱的抗乙酰胆碱酯酶活性。结果:弯柱唐松草(Thalictrumuncinulatum Franch.)、阔叶十大功劳(Mahnia bealei(Fort.)Steam.)、蚬壳花椒(Zanthoxylum dissitumHemsl.)、刺柄南星(Arisaema aspeiatum N.E.Brown)、一把伞南星(Arisaema erunescens(Wall.)Schott)、猫儿屎(Decaisnea insignis(Griff)Hook.f.et thoms)、虎耳草(Saxifraga stolonifera curt.)和西固凤仙花(Impot-iens notolopha Maxim.)的总生物碱提取物具有明显的乙酰胆碱酯酶抑制活性,其IC50值分别为2.3μg.mL-1、2.9μg.mL-1、3.5μg.mL-1、11.0μg.mL-1、16.9μg.mL-1、22.7μg.mL-1、25.3μg.mL-1和40.7μg.mL-1。其他植物的总生物碱表现出较弱或无乙酰胆碱酯酶抑制活性。结论:这8种植物的总生物碱对乙酰胆碱酯酶有较好的抑制活性,可进一步跟踪分离其中的活性成分。

Objective:To assess acetylcholinesterase(AChE) inhibitory activity of 22 species of plants total alkaloidal extracts which are collected from Wenxian and Zhouqu,Gansu Province for the further research for natural acetylcholinesterase inhibitors.Methods:The total alkaloids were extracted by acid and alkali aqueous solution treatment.The AChE inhibitory activity was determined by modified Ellman's colorimetric method in 96-well microplates.Results:The results showed that the total alkaloidal extracts from Thalictrum uncinulatum Franch.(Ranunculaceae),Mahnia bealei(Fort.) Steam.(Berberidaceae),Zanthoxylum dissitum Hemsl.(Rutaceae),Arisaema aspeiatum N.E.Brown(Araceae),Arisaema erunescens(Wall.) Schott(Araceae),Decaisnea insignis(Griff) Hook.f.et thoms(Lardizabalaceae),Saxifraga stolonifera curt.(Saxifragaceae) and Impotiens notolopha Maxim.(Balsaminaceae) exhibited remarkable AChE inhibitory activity with the IC50 values of 2.3μg·mL-1,2.9μg·mL-1,3.5μg·mL-1,11.0μg·mL-1,16.9μg·mL-1,22.7μg·mL-1,25.3μg·mL-1 and 40.7μg·mL-1,respectively.The rest of the alkaloidal extracts showed no or very weak AChE inhibitory activity.Conclusion:The total eight alkaloidal extracts are found to have strong activity against AChE,which can be further performed bio-guided isolation to obtain active compounds.