亚麻地上部分的木脂素成分及其活性  

Lignan constituents and activities of Linum usitatissimum L. above ground

作　　者：陈祥[1,2] 贾景明[1] 杨郁[2] 于能江 CHEN Xiang JIA Jing-ming YANG Yu YU Neng-jiang(School of Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China Institute of Pharmacology and Toxicology, Academy of Military Medicine Sciences, Beijing 100850, China)

机构地区：[1]沈阳药科大学,沈阳110016 [2]军事医学科学院毒物与药物研究所,北京100850

出　　处：《国际药学研究杂志》2017年第6期590-594,共5页Journal of International Pharmaceutical Research

基　　金：国家"重大新药创制"科技重大专项资助项目(2013ZX09102108);北京市科委资助课题(Z131100006513013)

摘　　要：目的研究亚麻科亚麻属植物亚麻地上部分的化学成分及其活性。方法综合运用硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱和半制备高效液相色谱等方法,对亚麻地上部分化学成分进行分离纯化。根据波谱数据以及旋光度数据对得到的化合物进行结构鉴定,并采用荧光素酶(luciferase)报告基因检测法测定化合物的活性。结果从亚麻地上部分分离得到8个低含量的二苄基丁内酯木脂素化合物,分别鉴定为:(-)-扁柏脂素(hinokinin,1)、(-)-bursehernin(2)、(-)-二甲基罗汉松脂素(dimethylmatairesinol,3)、(-)-yatein(4)、(-)-thujaplicatin trimethyl ether(5)、nemerosin(6)、(+)-E-7,8-去氧罗汉松脂素二甲酯(dehydromatairesinol dimethyl ether,7)和E-7,8-dehydrothujaplicatin trimethyl ether(8)。结论化合物7、8为首次从亚麻中分离得到,且化合物8为首次报道核磁共振波谱数据。活性评价结果显示化合物1和3对IL-6/STAT3信号转导通路的抑制活性较强,IC50值分别为42.12和43.43μmol/L。Objective To investigate the chemical constituents and activities of Linum usitatissimum L.aboveground. Methods The chemical constituents were separated through silica gel,ODS,Sephadex LH-20,and semi-preparative RP-HPLC chromatography and identified by optical rotation and spectroscopic analysis. All of the isolates were evaluated for their inhibitory activities by the luciferase assay. Results Eight dibenzylbutyrolactone lignans were separated from L. usitatissimum and identified as（-）-hinokinin（1）,（-）-bursehernin（2）,（-）-dimethylmatairesinol（3）,（-）-yatein（4）,（-）-thujaplicatin trimethyl ether（5）,nemerosin（6）,（＋）-E-7,8-dehydromatairesinol dimethyl ether（7）,and E-7,8-dehydrothujaplicatin trimethyl ether（8）,respectively. Conclusion Compounds 7 and 8 were isolated from L. usitatissimum for the first time,and NMR spectral data of compound 8 were reported for the first time. Compounds 1 and 3 showed moderate inhibitory activities on IL-6/STAT3 signaling pathway with IC50 values of 42.12 and 43.43 μmol/L,respectively.

关 键 词：亚麻 木脂素 结构鉴定 JAK/STAT抑制活性 

分 类 号：R284.1[医药卫生—中药学]