State Key Laboratory of Phytochemistry, Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, People's Republic of China.
J Nat Prod. 2013 May 24;76(5):896-902. doi: 10.1021/np4000262. Epub 2013 Apr 26.
Nine new triterpene derivatives, yunnanterpenes A-F (1-6), 15,16-seco-cimiterpenes A and B (7, 8), and cimilactone C (9), and 15 known analogues (10-24) were isolated from the aerial parts of Cimicifuga yunnanensis. The new structures were established using a combination of MS, NMR, and single-crystal X-ray diffraction techniques. WT MEFs (wild-type mouse embryonic fibroblasts) and tumorigenic cell lines p53(-/-)+H-RasV12 and p53(-/-)+p53(N236S)+H-RasV12 were used for evaluating active structures, targeting p53(N236S) (corresponding to p53(N239S) in humans) mutation. Compound 5 showed nonselective activities against these cell lines, with IC50 values of 5.8, 8.6, and 6.0 μM, respectively. Compound 4 exhibited greater selectivity against the p53(-/-)+p53(N236S)+H-RasV12 cells (IC50 5.5 μM) than against the WT MEFs cells (IC50 14.3 μM).
从云南升麻的地上部分分离得到了 9 种新的三萜衍生物,即 yunnanterpenes A-F(1-6)、15,16-裂环-cimicifugene A 和 B(7,8)以及 cimilactone C(9),以及 15 种已知类似物(10-24)。新结构是通过 MS、NMR 和单晶 X 射线衍射技术的组合确定的。WT MEFs(野生型小鼠胚胎成纤维细胞)和致瘤细胞系 p53(-/-)+H-RasV12 和 p53(-/-)+p53(N236S)+H-RasV12 用于评估针对 p53(N236S)(对应于人类的 p53(N239S))突变的活性结构。化合物 5 对这些细胞系表现出非选择性活性,其 IC50 值分别为 5.8、8.6 和 6.0 μM。化合物 4 对 p53(-/-)+p53(N236S)+H-RasV12 细胞(IC50 为 5.5 μM)的选择性大于对 WT MEFs 细胞(IC50 为 14.3 μM)。