冬凌草中三个新的对映-贝壳杉烷二萜及其细胞毒活性(英文)  

Three new ent-kaurane diterpenoids from Isodon rubescens and their cytotoxicities

作　　者：刘旭[1,2] 薛永波[1] 董可[1] 李小年[1] 李艳[1] 普建新[1] 吴继洲[2] 孙汉董[1] 

机构地区：[1]中国科学院植物昆明植物研究所化学与西部植物资源持续利用国家重点实验室,昆明650201 [2]华中科技大学同济药学院天然药物化学与资源评价湖北省重点实验室,武汉430030

出　　处：《中国天然药物》2012年第6期464-470,共7页

基　　金：supported by the NSFC-Joint Foundation of Yunnan Province (No. U0832602);the National Natural Science Foundation of China (No. 81172939);the Major State Basic Research Development Program of China (No.2009CB522300);the Reservation-Talent Project of Yunnan Province(2011CI043);the Major Direction Projection Foundation of CAS Intellectual Innovation Project (No. 2010KIBA05)~~

摘　　要：目的:研究产自湖北省建始县的冬凌草(Isodon rubescens)地上部分的化学成分; 方法:利用正反相硅胶柱色谱、高效液相色谱等现代分离技术进行分离; 通过IR,UV, MS, NMR等波谱方法鉴定了化合物结构式; 对化合物1进行了单晶X-射线衍射分析, 确定了其绝对构型; 化合物1–9进行了对HL-60, SMMC-7721, A-549, MCF-7和SW-480细胞株的体外细胞毒活性测定; 结果:分离鉴定了8个对映-贝壳杉烷二萜和1个对映-赤霉烷二萜; 结论:建始冬凌草庚素–壬素(1–3)为新化合物, 其中2是一个少见的、3位为半缩酮结构的3,20-环氧-对映-贝壳杉烷二萜; 所有受试化合物中, 4和5对某些细胞株表现出一定的体外抗增殖活性。AIM： To study the chemical constitutions of the aerial parts of Isodon rubescens in Jianshi county, Hubei Province, China. METHOD： Compounds 1-9 were isolated and purified by normal silica gel and Ci8 reversed phase silica gel column chromatography, and HPLC. Their structures were elucidated by extensive spectroscopic methods （IR, UV, MS and NMR）, and the absolute configuration of 1 was determined by single crystal X-ray diffraction. Compounds 1-9 were evaluated for their in vitro cytotoxicity against human tumor HL-60, SMMC-7721, A-549, MCF-7, and SW-480 cell lines. RESULT： Eight ent-kaurane diterpenoids and one ent-gibberellanoid were isolated and identified. CONCLUSIONS： Compounds 1-3 （jianshirubesins G-I） were new diterpenoids, of which 2 was a rare 3, 20-epoxy-ent-kaurane with a hemiketal at C-3. Among all of the diterpenoids tested, compounds 4 and 5 exhibited moderate inhibitory activity on the proliferation of certain cancer cells.

关 键 词：冬凌草 对映 贝壳杉烷二萜 细胞毒活性 建始冬凌草庚素一壬素 

分 类 号：R284.1[医药卫生—中药学]