State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China; Natural Products Chemistry Department, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China; University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China; School of Life Science and Technology, Shanghai Tech University, Shanghai 201210, People's Republic of China.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, People's Republic of China; University of Chinese Academy of Sciences, Beijing 100049, People's Republic of China; School of Life Science and Technology, Shanghai Tech University, Shanghai 201210, People's Republic of China.
Fitoterapia. 2018 Mar;125:174-183. doi: 10.1016/j.fitote.2018.01.007. Epub 2018 Feb 2.
A phytochemical investigation of twigs of Podocarpus nagi resulted in the identification of eight new type B nagilactones (1-8), all bearing a 7α,8α-epoxy-9(11)-enolide substructure, along with two known analogs (9-10). Their structures were determined on the basis of spectroscopic analysis, including HRESIMS, IR and NMR experiments, and X-ray crystallographic analysis. In vitro cytotoxic assay exhibited that compounds 1, 2, 9 and 10 could induce antiproliferation against three different types of human cancer cells while compounds 3 and 5 were inactive. Notably, the IC value of compound 1 is 0.208μM for A431 human epidermoid carcinoma cells, reaching the same level as the positive control combretastatin A-4 (0.104μM). Furthermore, compound 1 performed a strong inhibition of cancer cells by triggering apoptosis and arresting the cell cycle at G phase. These results unfold potential anticancer therapeutic applications of type B nagilactones.
对罗汉松科罗汉松属的嫩枝进行了植物化学研究，分离得到了 8 个新的 B 型罗汉松内酯（1-8），它们都含有 7α,8α-环氧-9(11)-烯内酯结构，此外还分离得到了两个已知的类似物（9-10）。通过波谱分析，包括高分辨质谱、红外和核磁共振实验以及 X 射线晶体学分析，确定了它们的结构。体外细胞毒性试验表明，化合物 1、2、9 和 10 对三种不同类型的人癌细胞具有抑制增殖活性，而化合物 3 和 5 则没有活性。值得注意的是，化合物 1 对 A431 人表皮样癌细胞的 IC 值为 0.208μM，与阳性对照药物 combretastatin A-4（0.104μM）相当。此外，化合物 1 通过诱导细胞凋亡和将细胞周期阻滞在 G 期，对癌细胞具有很强的抑制作用。这些结果表明 B 型罗汉松内酯具有潜在的抗癌治疗应用。
