Six new triterpene saponins (1–5,7) and 3 known saponins (6,8,9) were isolated from MeOH extracts of the cactus Stenocereus pruinosus. The structures of the isolated saponins were elucidated using MS, IR, and comprehensive NMR measurements. To develop drugs for treating Alzheimer’s disease (AD) on the basis of the amyloid cascade hypothesis, the isolated saponins were evaluated for inhibition of BACE1 activity and amyloid beta (Aβ) aggregation using thioflavin-T assay, and triterpenes as an aglycone moiety and an alkaline hydrolysate of the saponins were also evaluated. One saponin, stenoside A (7), exhibited inhibitory activity related to Aβ aggregation and its degree of Aβ aggregation was 40.6% at 100 μM.

Graphic abstract

中文翻译：

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仙人掌Stenocereus pruinosus中三萜皂苷的β淀粉样蛋白聚集抑制活性

从仙人掌Stenocereus pruinosus的 MeOH 提取物中分离出六种新的三萜皂苷 ( 1-5 , 7 )和 3 种已知的皂苷 ( 6 , 8 , 9 )。使用 MS、IR 和综合 NMR 测量阐明了分离的皂苷的结构。为了在淀粉样蛋白级联假说的基础上开发治疗阿尔茨海默病 (AD) 的药物，使用硫代黄素-T 测定法评估了分离的皂苷对 BACE1 活性和淀粉样蛋白 β (Aβ) 聚集的抑制作用，三萜类作为糖苷配基和还评价了皂苷的碱性水解产物。一种皂甙、 stenoside A ( 7)，表现出与 Aβ 聚集相关的抑制活性，其 Aβ 聚集程度在 100 μM 时为 40.6%。

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