Chen De-Li, Ma Guo-Xu, Yang Er-Lan, Yang Yun, Wang Can-Hong, Sun Zhao-Cui, Liang Han-Qiao, Xu Xu-Dong, Wei Jian-He
Hainan Branch Institute of Medicinal Plant Development (Hainan Provincial Key Laboratory of Resources Conservation and Development of Southern Medicine), Chinese Academy of Medical Sciences & Peking Union Medical College, Haikou 570311, China; Institute of Medicinal Plant Development (Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription, Chinese Academy of Medical Sciences), Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, China.
Institute of Medicinal Plant Development (Key Laboratory of New Drug Discovery Based on Classic Chinese Medicine Prescription, Chinese Academy of Medical Sciences), Chinese Academy of Medical Sciences & Peking Union Medical College, No. 151, Malianwa North Road, Haidian District, Beijing 100193, China.
Bioorg Chem. 2022 Oct;127:105982. doi: 10.1016/j.bioorg.2022.105982. Epub 2022 Jun 23.
Three new cadinane-type sesquiterpenoid dimeric diastereomers (1-3) named hibisceusones A-C were obtained from the infected stems of Hibiscus tiliaceus. The structures were determined by NMR spectroscopy and MS techniques, and the absolute configurations were assigned by ECD and single-crystal X-ray diffraction techniques. Compounds 1-3 are diastereomers, and contain a 1,4-dioxane ring linearly fused to different cadinane-type polycyclic skeletons. This is the first time that such a structure has been identified in natural products. Compounds 1-3 exhibited cytotoxic activities, and 2 showed a significantly high anti-triple-negative breast cancer (TNBC) effect. The anti-cancer effect of compound 2 was 3-4 fold higher than that of 1 and 3. The anti-cancer effect was generated via the induction of the apoptosis of the MDA-MB-231 cells by inhibiting the PI3Kα pathway.
从黄槿受感染的茎中获得了三种新的杜松烷型倍半萜二聚体非对映异构体（1-3），命名为木槿素A-C。通过核磁共振光谱和质谱技术确定了其结构，并通过电子圆二色光谱和单晶X射线衍射技术确定了绝对构型。化合物1-3为非对映异构体，含有一个与不同杜松烷型多环骨架线性稠合的1,4-二氧六环环。这是首次在天然产物中鉴定出这种结构。化合物1-3表现出细胞毒性活性，化合物2对三阴性乳腺癌（TNBC）显示出显著的高抗癌效果。化合物2的抗癌效果比化合物1和3高3-4倍。其抗癌作用是通过抑制PI3Kα途径诱导MDA-MB-231细胞凋亡而产生的。
