Huang Hung-Tse, Liaw Chia-Ching, Lin Yu-Chi, Liao Geng-You, Chao Chih-Hua, Chiou Chun-Tang, Kuo Yao-Haur, Lee Kung-Ta
Division of Chinese Materia Medica Development, National Research Institute of Chinese Medicine, Ministry of Health and Welfare, Taipei 11201, Taiwan.
Department of Biochemical Science and Technology, National Taiwan University, Taipei 10617, Taiwan.
Pharmaceuticals (Basel). 2021 Oct 29;14(11):1108. doi: 10.3390/ph14111108.
is a popular material used in foods and herbal medicines in Asia for clearing heat and resolving toxins. However, phytochemical research on this plant is very rare. In this study, eleven new diterpenoids, mesonols A-K (), comprising seven -kauranes, three -atisanes, and one sarcopetalane, were isolated from its methanolic extract. Structural elucidation of compounds was performed by spectroscopic methods, especially 2D NMR, HRESIMS, and X-ray crystallographic analysis. All isolates were assessed for their antiproliferative activity, and compounds showed potential antiproliferative activities against A549, Hep-3B, PC-3, HT29, and U937 cancer cells, with IC values ranging from 1.97 to 19.86 µM. The most active compounds, and , were selected for further investigation of their effects on cell cycle progression, apoptosis, and ROS generation in U937 human leukemia cancer cells. Interestingly, it was found that compounds and induced antiproliferative effects in U937 cells through different mechanisms. Compound caused cell cycle arrest at the G2/M phase and subsequent cell death in a dose- and time-dependent manner. However, -mediated antiproliferation of U937 cells triggered ROS-mediated mitochondrial-dependent apoptosis. These results provide insight into the molecular mechanism involved in the antiproliferative activities of compounds and in U937 cells. Altogether, the study showed that new diterpenoid compounds and from are potent and promising anticancer agents.
是亚洲食品和草药中常用的一种用于清热和解毒的材料。然而，对这种植物的植物化学研究非常罕见。在本研究中，从其甲醇提取物中分离出11种新的二萜类化合物，即介子醇A - K（），包括7种贝壳杉烷型、3种乌苏烷型和1种肉托果烷型。通过光谱方法，特别是二维核磁共振、高分辨电喷雾电离质谱和X射线晶体学分析对化合物进行结构解析。对所有分离物进行抗增殖活性评估，化合物对A549、Hep - 3B、PC - 3、HT29和U937癌细胞显示出潜在的抗增殖活性，IC值范围为1.97至19.86 μM。选择活性最强的化合物和，进一步研究它们对U937人白血病癌细胞的细胞周期进程、凋亡和活性氧生成的影响。有趣的是，发现化合物和通过不同机制在U937细胞中诱导抗增殖作用。化合物导致细胞周期停滞在G2/M期，并随后以剂量和时间依赖性方式导致细胞死亡。然而，介导的U937细胞抗增殖作用触发了活性氧介导的线粒体依赖性凋亡。这些结果为化合物和在U937细胞中的抗增殖活性所涉及的分子机制提供了见解。总之，该研究表明来自的新二萜类化合物和是有效的、有前景的抗癌剂。
