大戟脂中二萜类成分及细胞毒活性研究  

Diterpenes from Euphorbium and their cytotoxicity

作　　者：王书云 李钦[1] 李国玉[4] 张珂 梁宏刚 黄超 黄健 王金辉[2,3,4] 杨宝峰[2] WANG Shuyun;LI Qin;LI Guoyu;ZHANG Ke;LIANG Honggang;HUANG Chao;HUANG Jian;WANG Jinhui;YANG Baofeng(School of Pharmacy, Henan University, Kaifeng 475004, China;Department of Medicinal Chemistry and Natural Medicine Chemistry/State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Harbin Medical University, Harbin 150081, China;School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China;School of Pharmacy, Shihezi University/Key Laboratory of Xinjiang Phytomedicine Resource and Utilization, Ministry of Education, Shihezi 832001, China)

机构地区：[1]河南大学药学院,河南开封475004 [2]哈尔滨医科大学药化教研室/省部共建生物医药工程重点实验室,哈尔滨150081 [3]沈阳药科大学中药学院,沈阳10016 [4]石河子大学药学院/新疆植物药资源利用教育部重点实验室,新疆石河子832001

出　　处：《河南大学学报（医学版）》2019年第3期153-157,165,共6页Journal of Henan University:Medical Science

基　　金：国家科学与技术支撑计划重点项目(2012BAI30B02);国家“重大新药创制”科技重大专项(2018ZX09305005)

摘　　要：〔目的〕研究大戟脂中二萜类抗肿瘤活性成分。〔方法〕通过硅胶柱色谱、ODS柱色谱和RP-HPLC等方法,从大戟脂的甲醇提取物中共分离得到5个二萜类化合物,利用各种波谱学手段及理化性质确定化合物的结构。对分离得到的二萜类化合物的生合成途径进行了简单推测,并采用MTT法对分离得到的单体化合物进行细胞毒活性测试。〔结果〕分离得到的5个二萜类化合物包括3个Ingol烷型二萜、2个巴豆烷型二萜,分别鉴定为:ingol7,8,12-triacetate-3-(4-me-thoxy-phenyl)acetate(1)、ingol7,8,12-triacetate-3-phenylacetate(2)、ingol3,8,12-triacetate(3)、12-deoxyphorbol-13-isobu-tyrate-20-acetate(4)、12-deoxyphorbol-13-angelate-20-acetate(5)。〔结论〕化合物1~3是首次从该植物中分离得到,并对C6细胞株有较强的细胞毒活性。Objective〕To study the antitumor active constituents of diterpenes from Euphorbium.〔Methods〕By means of various chromatographic methods such as silica gel, ODS and semi-preparative HPLC, five compounds were isolated from the methanol extraction of Euphorbium. Their structures were identified by spectroscopic methods and physicochemical properties. In addition, putative biogenetic relationships to these compounds were proposed and MTT assay was used to evaluate the compounds.〔Results〕The compounds include three ingol-type and two tigliane-type diterpenoids. These isolated compounds were identified as ingol 7,8,12-triacetate-3-(4-methoxy-phenyl) acetate (1), ingol 7,8,12-triacetate-3-phenylacetate (2), ingol 3,8,12-triacetate (3), 12-deoxyphorbol-13-isobutyrate-20-acetate (4), 12-deoxyphorbol-13-angelate-20-acetate (5).〔Conclusion〕Compounds 1 ~ 3 were firstly isolated from the plant and showed strong cytotoxic activity to C6 cell lines.

关 键 词：维药 大戟脂 二萜 生合成 细胞毒活性 

分 类 号：R285.1[医药卫生—中药学]