School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.
Evid Based Complement Alternat Med. 2014;2014:524650. doi: 10.1155/2014/524650. Epub 2014 Apr 17.
Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment. Cholinesterase inhibitors are widely used for the symptomatic treatment of Alzheimer's disease to enhance central cholinergic transmission. In this study, a bioactivity-oriented screening platform based on a modified Ellman's method and HPLC-QTOF MS technique was developed to rapidly screen active agents of Anemarrhena asphodeloides Bge. The 60% ethanol fraction from an ethyl acetate extract exhibited the most potential anticholinesterase activity. Fifteen steroid saponins were identified by the mass spectrum, standards and literature reports. Twenty-five compounds were isolated from the active fraction. The results showed that compounds with the C6-C3-C6 skeleton probably had both AChE and BuChE inhibitory activities. Xanthone and benzene derivatives exhibited no or little activity. Lignans showed weak BuChE inhibitory activity. The steroidal saponins demonstrated moderate or weak AChE inhibitory activity.
阿尔茨海默病（AD）是一种神经退行性疾病，其特征是进行性记忆丧失和认知障碍。乙酰胆碱酯酶抑制剂被广泛用于 AD 的症状治疗，以增强中枢胆碱能传递。在这项研究中，建立了一个基于改良 Ellman 法和 HPLC-QTOF MS 技术的基于生物活性的筛选平台，用于快速筛选知母的活性成分。乙酸乙酯提取物的 60%乙醇级分表现出最有潜力的抗乙酰胆碱酯酶活性。通过质谱、标准品和文献报道鉴定了 15 个甾体皂苷。从活性部分分离出 25 种化合物。结果表明，具有 C6-C3-C6 骨架的化合物可能具有 AChE 和 BuChE 抑制活性。酮和苯衍生物表现出无或很少的活性。木脂素表现出弱的 BuChE 抑制活性。甾体皂苷表现出中等或弱的 AChE 抑制活性。
