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来自多刺仙人掌的三萜皂苷的淀粉样β聚集抑制活性。

Amyloid β aggregation inhibitory activity of triterpene saponins from the cactus Stenocereus pruinosus.

机构信息

Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose-shi, Tokyo, 204-8588, Japan.

出版信息

J Nat Med. 2021 Mar;75(2):284-298. doi: 10.1007/s11418-020-01463-0. Epub 2020 Nov 24.

Abstract

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.

摘要

从刺梨仙人掌茎提取物的甲醇提取物中分离得到了六种新的三萜皂苷(1-5、7)和三种已知的皂苷(6、8、9)。通过 MS、IR 和综合 NMR 测量确定了分离的皂苷的结构。为了根据淀粉样蛋白级联假说开发治疗阿尔茨海默病(AD)的药物,使用噻唑蓝-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,并且还评估了三萜作为糖苷配基和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,其在 100 μM 时 Aβ聚集程度为 40.6%。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/52e5/7684148/32d7f787a89c/11418_2020_1463_Fig1_HTML.jpg

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