靶向亲和-液相色谱-质谱联用技术快速筛选黄藤总生物碱中乙酰胆碱酯酶抑制剂

采用靶向亲和-液相色谱-质谱联用技术(Target molecule affinity-LC-ESI-MSn)快速筛选黄藤总生物碱中能够抑制乙酰胆碱酯酶活性的成分,共筛选出12种具有潜在抑制乙酰胆碱酯酶的活性成分,并鉴定了6种成分,分别为黄藤素(Palmatine)、小檗碱(Berberine)、药根碱(Jatrorrhizine)、巴马汀红碱(Palmatrubine)、7,8-二氢-8-羟基小檗碱(7,8-Dihydro-8-hydroxyberberine)、Groenlandicine,结合体外酶学实验对这6种化合物进行了活性验证实验.结果表明,黄藤素抑制活性最强,其抑制作用强于阳性对照药盐酸多奈哌齐,说明黄藤素具有开发成抗阿尔茨海默症药物的潜力.本方法简单、快速、准确地从复杂的中药提取物中筛选出具有抑制乙酰胆碱酯酶活性的成分,适用于复杂体系中的高通量筛选.

Screening and Structure Characterization of Acetylcholinesterase Inhibitors from Total Alkaloids of Fibraurea recisa Pierre.by Target Molecule Affinity-Liquid Chromatography-Tandem Mass Spectrometry

A target molecule affinity-ultrafiltration liquid chromatography-electrospray ionization tandem mass spectrometric (LC-ESI-MSn) method was established for rapid screening acetylcholinesterase (AChE) inhibitors from total alkaloids of fibraurea recisa Pierre.A total of 12 potential inhibitors were screened from Fibraurea recisa Pierre.and 6 compounds were identified including palmatine,berberine,jatrorrhizine,palmatrubine,7,8-dihydro-8-hydroxyberberine and groenlandicine.The AChE inhibitory activity of these 6 compounds was validated in vitro.Palmatine showed the strongest inhibitory activity for AChE,which was stronger than that of donepezil hydrochloride,demonstrating the potential of palmatine as anti-Alzheimer's drug.This method is simple,rapid,and accurate for directly screening active ingredients which can inhibit AChE from complex extract of traditional Chinese medicines.