刺五加根茎活性成分对蛋白酪氨酸磷酸酶1B的抑制作用  

Inhibitory Effect of Active Ingredient from Rhizomes of Acanthopanax senticosus on Protein Tyrosine Phosphatase 1B

作　　者：车环宇 赵凌志[2] 孙连双 董洪坤 滕国生 CHE Huanyu;ZHAO Lingzhi;SUN Lianshuang;DONG Hongkun;TENG Guosheng(School of Medicine,Tonghua Normal University,Tonghua 134002,Jilin Province,China;The Second Hospital of Jilin University,Changchun 130041,China;School of Chemistry and Life Science,Changchun University Technology,Changchun 130012,China)

机构地区：[1]通化师范学院医药学院,吉林通化134002 [2]吉林大学第二医院,长春130041 [3]长春工业大学化学与生命科学学院,长春130012

出　　处：《吉林大学学报（理学版）》2019年第2期438-444,共7页Journal of Jilin University:Science Edition

基　　金：吉林省教育厅"十三五"科学技术研究项目(批准号:2016-351)

摘　　要：采用正相硅胶柱色谱、C-18反相柱色谱和半制备型高效液相色谱(HPLC)等多种层析方法分离、纯化刺五加根茎乙酸乙酯层中的降糖活性成分,得到10个化合物,通过核磁共振氢谱(1 H-NMR)、核磁共振碳谱(13C-NMR)、无畸变极化转换技术(DEPT)、质谱(MS)等方法分析各化合物的光谱数据,并与相关文献比较,确定所得化合物的结构,对其进行活性测试.结果表明:化合物1～5为贝壳杉烷型二萜类化合物,化合物6～8为松脂烷型二萜类化合物,化合物9,10为木脂素类化合物;化合物1,5,7,8对蛋白酪氨酸磷酸酶1B(PTP1B)具有明显的特异性抑制活性,化合物2,4,9对蛋白磷酸酶(PP1)具有较好的抑制活性,化合物9,10对牛痘H1相关磷酸酶(VHR)的抑制活性作用较低.The hypoglycemic active ingredient in the ethyl acetate layer of rhizome of Acanthopanax senticosus was separated and purified by normal phase silica gel column chromatography,C-18 reverse phase column chromatography and semi-preparative high performance liquid chromatography(HPLC).Ten compounds were obtained,and the structures of the obtained compounds were determined by analyzing spectral data of nuclear magnetic resonance hydrogen spectroscopy(^1H-NMR),nuclear magnetic resonance carbon spectroscopy(^13 C-NMR),distortionless enhancement by polarization transfer(DEPT),mass spectrum(MS),and compared with the relevant literatures.Their activities were tested.The results show that compounds 1-5 are kaurane-type diterpenoids,compounds 6-8 are turpentine-type diterpenoids,and compounds 9,10 are lignin compounds.Compounds 1,5,7,8 have significant specific inhibitory activity on protein tyrosine phosphatase 1B(PTP1B),compounds 2,4,9 have good inhibitory effects on protein phosphatase 1(PP1),and compounds 9,10 have a low inhibitory effect on vaccinia H1 related(VHR)phosphatase.

关 键 词：刺五加 活性成分 蛋白酪氨酸磷酸酶1B 糖尿病 

分 类 号：R965.1[医药卫生—药理学]