罗汉果是我国首批批准的药食同源品种之一，已被用作食品工业的天然甜味剂和止咳化痰的传统药物。然而，每年都有大量的罗汉果根被丢弃，造成了资源的极大浪费。从罗汉果的根中分离出 12 种未描述的去甲葫芦素型三萜糖苷、siraitiaosides A-L (1-12) 和 6 种已知类似物 (13-18)。通过综合数据分析，包括 HRESIMS、UV、IR、NMR、ECD 计算和 X 射线晶体学分析，阐明了分离的去甲葫芦素糖苷的结构。 Siraitiaosides A-E (1-5) 具有不寻常的 19,29-降葫芦素框架，而 siraitiaosides F-L (6-12) 具有罕见的 29-降葫芦素框架。值得注意的是，化合物 4 显示出中等的抗乙酰胆碱酯酶 (AChE) 活性，IC50 为 21.0 μM，同时，化合物 16 和 18 对 MCF-7、CNE-1 和 HeLa 癌细胞系表现出显着的细胞毒活性，IC50 值为 2.1- 15.2μM。计算机模拟研究表明，化合物 4 与 AChE 紧密结合，结合能为-5.04 kcal/mol，化合物 18 可以与自噬、细胞凋亡、迁移/侵袭等相关的 PI3K、AKT1、ERK2 和 MMP9 蛋白紧密结合。生长/增殖。综上所述，罗汉果的根部含有多种生物活性成分，具有潜在的药用价值。版权所有 © 2024。由 Elsevier Ltd 出版。

Siraitia grosvenorii Swingle is one of the first approved medicine food homology species in China, and it has been used as a natural sweetener in the food industry and as a traditional medicine to relieve cough and reduce phlegm. However, many S. grosvenorii roots are discarded yearly, which results in a great waste of resources. Twelve undescribed norcucurbitacin-type triterpenoid glycosides, siraitiaosides A-L (1-12), and six known analogs (13-18) were isolated from the roots of S. grosvenorii. The structures of isolated norcucurbitacin glycosides were elucidated by comprehensive data analyses, including HRESIMS, UV, IR, NMR, ECD calculations, and X-ray crystallography analysis. Siraitiaosides A-E (1-5) featured an unusual 19,29-norcucurbitacin framework while siraitiaosides F-L (6-12) featured a rare 29-norcucurbitacin framework. Notably, compound 4 displayed moderate anti-acetylcholinesterase (AChE) activity with an IC50 of 21.0 μM, meanwhile, compounds 16 and 18 exhibited pronounced cytotoxic activities against MCF-7, CNE-1, and HeLa cancer cell lines with IC50 values of 2.1-15.2 μM. In silico studies showed that compound 4 bound closely to AChE with a binding energy of -5.04 kcal/mol, and compound 18 could tightly bind to PI3K, AKT1, ERK2, and MMP9 proteins that related to autophagy, apoptosis, migration/invasion, and growth/proliferation. In summary, the roots of Siraitia grosvenorii have potential medicinal values due to the multiple bioactive components.Copyright © 2024. Published by Elsevier Ltd.