College of Chemistry and Pharmaceutical Science, Qingdao Agricultural University, Changcheng Rd, Chengyang district, Qingdao 266109, China.
School of Pharmaceutical Sciences, Wenzhou Medical University, Wenzhou 325035, China.
Mar Drugs. 2018 Mar 14;16(3):94. doi: 10.3390/md16030094.
The human β-site amyloid cleaving enzyme (BACE1) has been considered as an effective drug target for treatment of Alzheimer's disease (AD). In this study, , which is a Far East specialty food known as innkeeper worm, ethanol extract was studied by bioassay-directed fractionation and isolation to examine its potential β-site amyloid cleaving enzyme inhibitory and antimicrobial activity. The following compounds were characterized: hecogenin, cholest-4--3-one, cholesta-4,6--3-ol, and hurgadacin. These compounds were identified by their mass spectrometry, ¹H, and C NMR spectral data, comparing those data with NIST/EPA/NIH Mass spectral database (NIST11) and published values. Hecogenin and cholest-4--3-one showed significant inhibitory activity against BACE1 with EC values of 116.3 and 390.6 µM, respectively. Cholesta-4,6--3-ol and hurgadacin showed broad spectrum antimicrobial activity, particularly strongly against , , , and , with minimal inhibitory concentration (MIC) ranging from 0.46 to 0.94 mg/mL. This is the first report regarding those four known compounds that were isolated from and their anti-BACE1 and antimicrobial activity, highlighting the fact that known natural compounds may be a critical source of new medicine leads. These findings provide scientific evidence for potential application of those bioactive compounds for the development of AD drugs and antimicrobial agents.
人β-淀粉样肽裂解酶（BACE1）已被认为是治疗阿尔茨海默病（AD）的有效药物靶点。在这项研究中，远东特产食品“知更虫”的乙醇提取物通过基于生物测定的分步分离和分离进行了研究，以检查其潜在的β-淀粉样肽裂解酶抑制和抗菌活性。鉴定出以下化合物：海柯皂苷元、胆甾-4-烯-3-酮、胆甾-4,6-二烯-3-醇和 hurgadacin。这些化合物通过质谱、1H 和 C NMR 光谱数据进行了鉴定，通过将这些数据与 NIST/EPA/NIH 质谱数据库（NIST11）和已发表的值进行比较。海柯皂苷元和胆甾-4-烯-3-酮对 BACE1 表现出显著的抑制活性，EC 值分别为 116.3 和 390.6 μM。胆甾-4,6-二烯-3-醇和 hurgadacin 表现出广谱抗菌活性，特别是对 、 、 、 和 具有很强的抑制作用，最小抑菌浓度（MIC）范围为 0.46 至 0.94 mg/mL。这是首次从 中分离出这四种已知化合物及其抗 BACE1 和抗菌活性的报道，突出了已知天然化合物可能是新药物先导物的重要来源。这些发现为这些生物活性化合物在开发 AD 药物和抗菌剂方面的潜在应用提供了科学依据。
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