Journal of Natural Medicines ( IF 2.5 ) Pub Date : 2020-11-24 , DOI: 10.1007/s11418-020-01463-0 Koji Fujihara 1 , Takuya Shimoyama 1 , Ryo Kawazu 1 , Hiroaki Sasaki 1 , Kiyotaka Koyama 1 , Kunio Takahashi 1 , Kaoru Kinoshita 1
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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：
仙人掌三萜皂苷对β淀粉样蛋白聚集的抑制活性
从仙人掌Stenocereus pruinosus的甲醇提取物中分离出 6 个新的三萜皂苷 ( 1 – 5 , 7 ) 和 3 个已知的皂苷( 6,8,9 )。使用 MS、IR 和综合 NMR 测量阐明了分离的皂苷的结构。为了开发基于淀粉样蛋白级联假说的治疗阿尔茨海默病 (AD) 的药物，使用硫黄素-T 测定法评估分离的皂苷对 BACE1 活性和淀粉样蛋白 β (Aβ) 聚集的抑制作用，并使用三萜作为苷元部分和还评估了皂苷的碱性水解产物。一种皂苷 Stenoside A ( 7 ) 表现出与 Aβ 聚集相关的抑制活性，其 Aβ 聚集度在 100 μM 时为 40.6%。
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