Suppr超能文献

云南升麻地上部分的三萜及其对 p53(N236S)小鼠胚胎成纤维细胞的抗增殖作用。

Triterpenes from the aerial parts of Cimicifuga yunnanensis and their antiproliferative effects on p53(N236S) mouse embryonic fibroblasts.

机构信息

State Key Laboratory of Phytochemistry, Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming, People's Republic of China.

出版信息

J Nat Prod. 2013 May 24;76(5):896-902. doi: 10.1021/np4000262. Epub 2013 Apr 26.

Abstract

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).

摘要

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)。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验