威氏鼠尾草中的细胞毒贝壳杉烷二萜。

Cytotoxic ent-kaurane diterpenoids from Isodon wikstroemioides.

机构信息

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences , Kunming 650201, People's Republic of China.

出版信息

J Nat Prod. 2014 Apr 25;77(4):931-41. doi: 10.1021/np4010135. Epub 2014 Apr 3.

DOI:10.1021/np4010135

PMID:24697496

Abstract

Phytochemical investigation of EtOAc extracts of the aerial parts of Isodon wikstroemioides afforded 18 new ent-kaurane diterpenoids (wikstroemioidins E-V, 1-18), along with 17 known analogues (19-35). The absolute configurations of 1 and 16 were confirmed by single-crystal X-ray diffraction analysis. The isolates were screened against five human tumor cell lines; compounds 3, 4, 9, 11-13, 23, 25-28, and 33 exhibited significant cytotoxic activity against all five, with IC50 values ranging from 0.4 to 5.1 μM. In addition, 17 of the isolates strongly inhibited nitric oxide production in LPS-activated RAW264.7 macrophages.

摘要

从 Isodon wikstroemioides 的地上部分的 EtOAc 提取物中进行植物化学研究，得到了 18 个新的 ent-贝壳杉烷二萜（wikstroemioidins E-V，1-18），以及 17 个已知类似物（19-35）。通过单晶 X 射线衍射分析确定了 1 和 16 的绝对构型。对分离物进行了针对五种人肿瘤细胞系的筛选；化合物 3、4、9、11-13、23、25-28 和 33 对所有五种细胞均表现出显著的细胞毒性活性，IC50 值范围为 0.4 至 5.1 μM。此外，17 种分离物强烈抑制 LPS 激活的 RAW264.7 巨噬细胞中的一氧化氮产生。