School of Biological Science and Technology, University of Jinan, Jinan 250022, China.
Key Laboratory of Marine Mineral Resources and Polar Geology (Ministry of Education), School of Ocean Sciences, China University of Geosciences, Beijing 100083, China.
Fitoterapia. 2024 Jul;176:106029. doi: 10.1016/j.fitote.2024.106029. Epub 2024 May 19.
An intensive phytochemical investigation into the fruits of Schisandra chinensis afforded 28 triterpenoids incorporating diverse backbones with methyl-migration, ring-expansion and ring-opening features. Among them, ten compounds (1-10) including three likely extracting artefacts (8-10) were described for the first time. Their structures were fully characterized by comprehensive spectroscopic analyses, with the absolute configurations established via electronic circular dichroism and Mosher's NMR techniques. Preliminary biological evaluations revealed that nine isolates showed inhibitory activity against the hyperglycemic target α-glycosidase and 12 compounds exerted cytotoxicity toward three female tumor cell lines (Hela (cervical), MDA-MB231 and MCF-7 (breast)). Compound 6 exhibited the most promising potency on all the three tested cancer cells, and further assessment demonstrated that it could induce significant cell apoptosis and cycle arrest, as well as suppress cell migration, by regulating relevant proteins in MDA-MB231 cells.
对五味子果实进行了深入的植物化学研究，从中分离得到了 28 种具有不同骨架的三萜类化合物，包括甲基迁移、环扩张和环开裂等特征。其中，有 10 种化合物（1-10）包括 3 种可能的提取产物（8-10）是首次被描述的。通过全面的光谱分析，结合电子圆二色谱和 Mosher 的 NMR 技术，确定了它们的结构。初步的生物活性评价表明，有 9 种分离物对高血糖靶点 α-糖苷酶具有抑制活性，有 12 种化合物对三种女性肿瘤细胞系（宫颈癌细胞系 Hela、MDA-MB231 和 MCF-7）具有细胞毒性。化合物 6 在所有三种测试的癌细胞中表现出最有前途的活性，进一步的评估表明，它可以通过调节 MDA-MB231 细胞中的相关蛋白，诱导显著的细胞凋亡和细胞周期停滞，并抑制细胞迁移。
