痛安注射液的化学成分研究(Ⅰ)  

Chemical Constituents from Tong An Injection (Ⅰ)

作　　者：尚婵 李海波[2] 李孟璇[2] 苏真真[2] 孟兆青[2] 黄文哲[2] 王振中[2] 丁岗[2] 杨中林[2] 萧伟[2] 无 Shang Chan Li Haibo Li Mengxuan Su Zhenzhen Meng Zhaoqing Huang Wenzhe Wang Zhenzhong Ding Gang Yang Zhonglin Xiao Wei(China Pharmaceutical University, Nanjing 211198, China Jiangsu Kanion Parmaceutical Co. Ltd., Lianyungang 222001, China State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process, Lianyungang 222001, China)

机构地区：[1]中国药科大学中药学院,南京211198 [2]江苏康缘药业股份有限公司,连云港222001 [3]中药制药过程新技术国家重点实验室

出　　处：《世界科学技术-中医药现代化》2016年第12期2118-2124,共7页Modernization of Traditional Chinese Medicine and Materia Medica-World Science and Technology

基　　金：江苏省自然科学基金委青年基金项目(BK20140441):基于活性成分追踪分离及快速检识分析新策略的中药复方药效物质基础研究,负责人:李海波

摘　　要：目的:研究痛安注射液中的抗炎活性成分。方法:采用LPS诱导的RAW 264.7巨噬细胞炎症模型检测化合物对PGE_2抑制活性,综合应用HP-20大孔吸附树脂、硅胶柱色谱、ODS柱色谱、Sephadex LH-20柱色谱、制备及半制备HPLC等色谱方法对活性部位进行分离和纯化,根据化合物的光谱数据和理化性质鉴定化合物的结构。结果:痛安注射液中经HP-20大孔吸附树脂,95%乙醇洗脱部位为抗PGE_2释放活性部位,从中分离得到17个化合物,分别鉴定为丁香脂素(1)、N-反式阿魏酰酪胺(2)、白屈菜红碱(3)、青藤碱(4)、黄连碱(5)、血根碱(6)、白屈菜碱(7)、木兰花碱(8)、别隐品碱(9)、原阿片碱(10)、杜鹃素(11)、二氢血根碱(12)、Heptadec-(9Z)-enoic acid(13)、绿原酸(14)、隐绿原酸(15)、3,5-O-二咖啡酰奎宁酸(16)、4,5-O-二咖啡酰奎宁酸(17);通过PGE_2抑制活性检测,6个化合物对PGE_2具有很好的抑制作用。结论:化合物1-17均为首次从痛安注射液中分离得到,化合物2、5、9、10、11、12对PGE_2具有很好的抑制作用。This study aimed at investigating the antiviral constituents from the active fractions of Tong-An（TA） injection. In this study, the active constituents of TA injection were screened by LPS-induced PGE2 production mode to detect the contents of PGE2. The chemical constituents were isolated by HP-20 macroporous resin, silica gel column chromatography, ODS column chromatography, Sephadex LH-20 column chromatography and preparative and semi-preparative HPLC. The structures were identified by spectral data and physicochemical property. As a result, the 95% ethanol eluate of TA injection on the macroporous adsorption resin column was proved to be the active fraction of TA injection. Seventeen compounds were isolated from TA injection and identified as syringaresinol（1）, N-Trans-Feruloyltyramine（2）, chelerythrine（3）, sinomenine（4）,coptisine（5）, sanguinarine（6）, chelidoniny（7）, magnoflorine（8）, allocryptopine（9）, protopine（10）, farrerol（11）, dihydrosanguinarine（12）, heptadec-（9Z）-enoic acid（13）, chlorogenic acid（14）, cryptochlorogenin acid（15）, 3,5-di-O-caffeoylquinic acid（16） and 4,5-di-O-caffeoylquinic acid（17）. PGE2 inhibitory activities of these compounds were determined, among which six compounds presented inhibitory activities against PGE2. It was concluded that all the isolated compounds from TA injection were firstly reported with the favorable inhibitory activities of compounds 2, 5, 9, 10, 11, 12 against PGE2.

关 键 词：痛安注射液 黄酮 生物碱 有机酸 苯丙素 PGE2 

分 类 号：R284.1[医药卫生—中药学]