School of Biological Science and Technology, University of Jinan, Jinan, China.
Key Laboratory of Natural Pharmaceutical Chemistry, Shandong University of Traditional Chinese Medicine, Jinan, China.
Nat Prod Res. 2021 Sep;35(18):3004-3010. doi: 10.1080/14786419.2019.1682579. Epub 2019 Nov 1.
A novel monoterpenoid indole alkaloid, melognine () possessing an unprecedented skeleton with a 6/6/5/5/6/6 hexatomic rearranged ring system was isolated from the stems of . The structure with absolute configuration of was established by extensive spectroscopic analyses and quantum ECD calculations. Melognine showed significant cytotoxicity on human breast cancer BT549 cells with an IC value of 1.49 μM by MTT assay. Further mechanism of action study indicated that melognine demonstrated the ability to induce apoptosis by activation of caspase-3 and p53, and downregulation of Bcl-2 in BT549 cells.
从 中分离得到了一种新型的单萜吲哚生物碱,麦罗宁(),它具有前所未有的骨架,具有 6/6/5/5/6/6 个六原子重排的环系。通过广泛的光谱分析和量子 ECD 计算确定了麦罗宁的绝对构型。麦罗宁通过 MTT 分析在人乳腺癌 BT549 细胞中表现出显著的细胞毒性,IC 值为 1.49μM。进一步的作用机制研究表明,麦罗宁通过激活 caspase-3 和 p53,以及下调 BT549 细胞中的 Bcl-2,表现出诱导细胞凋亡的能力。