板蓝根乙醇提取物中生物碱类化学成分研究  

Study on alkaloids from alcohol extract of Radix Isatidis

作　　者：张东东 阮德清 李婧伊 陈凯先[1] 李医明[1] 王瑞[1] ZHANG Dong-dong;RUAN De-qing;LI Jing-yi;CHEN Kai-xian;LI Yi-ming;WANG Rui(Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China)

机构地区：[1]上海中医药大学,上海201203

出　　处：《中华中医药杂志》2020年第5期2287-2291,共5页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：国家自然科学基金项目(No.81573571,No.81673570);上海市科学技术委员会科研计划项目(No.15DZ0502601);上海市优秀学术带头人项目(No.16XD1403500)。

摘　　要：目的:研究板蓝根乙醇提取物中的生物碱化学成分及其抑制一氧化氮(NO)活性。方法:利用硅胶、反相ODS C18、葡聚糖凝胶等柱色谱以及半制备液相色谱等技术分离纯化,通过1D/2D-NMR、MS、IR等波谱学技术解析结构,采用LPS刺激产生的RAW264.7巨噬细胞测定所得化合物的NO抑制活性。结果:共分离鉴定了7个生物碱类成分,分别为菘蓝苷E(1)、3H-吲哚-3-酮(2)、(S)-(-)-spirobrassinin(3)、二氢新抗坏血酸原(4)、1-(3-indolyl)-2R,3-dihydroxypropan-1-one(5)、cephalanthrin A(6)和deoxyvasicinone(7),化合物1抑制NO释放活性的IC50值为57.6μmol/L。结论:1为新化合物且表现出温和的NO抑制活性,3为新天然产物,2、5和6首次从板蓝根中分离鉴定。Objective: To study the alkaloids of an alcohol extract of the Radix Isatidis and their nitric oxide(NO) inhibitory activities. Methods: The chemical components were isolated and purified by silica gel, sephadex LH-20, ODS C18 gel and semi preparative-HPLC chromatographic techniques, the structures were determined by 1 D/2 D-NMR, MS and IR spectral data analysis and the NO inhibitory activities were assessed based on LPS-stimulated RAW264.7 macrophages. Results: Seven alkaloids were obtained and elucidated as isatindigoside E(1), 3 H-indol-3-one(2),(S)-(-)-spirobrassinin(3), dihydroneoascorbigen(4), 1-(3-indolyl)-2 R, 3-dihydroxypropan-1-one(5), cephalanthrin A(6) and deoxyvasicinone(7), and compound 1 showed NO inhibitory activity with IC50 value of 57.6μmol/L. Conclusion: Isatindigoside E(1) is a new indole alkaloid glycoside which possesses moderate NO inhibitory activity, compound 3 is determined as a new natural product, while 2, 5 and 6 are isolated from the plant for the first time.

关 键 词：板蓝根 生物碱类化合物 菘蓝苷E 一氧化氮抑制活性 结构鉴定 

分 类 号：R284.1[医药卫生—中药学]