刺五加根茎活性成分对蛋白酪氨酸磷酸酶1B的抑制作用

吉林大学学报(理学版) ›› 2019, Vol. 57 ›› Issue (2): 438-444.

刺五加根茎活性成分对蛋白酪氨酸磷酸酶1B的抑制作用

车环宇¹, 赵凌志², 孙连双¹, 董洪坤¹, 滕国生^1,3

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

收稿日期:2018-04-18 出版日期:2019-03-26 发布日期:2019-03-26
通讯作者: 滕国生 E-mail:gshteng @163.com

Inhibitory Effect of Active Ingredient from Rhizomes of Acanthopanax senticosus on Protein Tyrosine Phosphatase 1B#br#

CHE Huanyu^1, ZHAO Lingzhi^2, SUN Lianshuang^1, DONG Hongkun^1, TENG Guosheng^1,3#br#

1. School of Medicine, Tonghua Normal University, Tonghua 134002, Jilin Province, China；2. The Second Hospital of Jilin University, Changchun 130041， China;3. School of Chemistry and Life Science, Changchun University Technology, Changchun 130012， China

Received:2018-04-18 Online:2019-03-26 Published:2019-03-26
Contact: TENG Guosheng E-mail:gshteng @163.com

摘要/Abstract

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(¹H-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.

关键词: 刺五加, 活性成分, 蛋白酪氨酸磷酸酶1B, 糖尿病

Abstract: 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 obtai
ned 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 spect
rum (MS), and compared with the relevant literatures. Their activities were tested. The results show that compounds 〖STHZ〗1
〖ST〗—〖STHZ〗5〖ST〗 are kauranetype diterpenoids, compounds 〖STHZ〗6〖ST
〗—〖STHZ〗8〖ST〗 are turpentinetype diterpenoids, and compounds 〖STHZ〗9〖
ST〗,〖STHZ〗10〖ST〗 are lignin compounds. Compounds 〖STHZ〗1〖ST〗,〖STHZ〗5〖ST〗,〖STHZ〗7〖ST〗,〖STHZ〗8〖ST〗 h
ave significant specific inhibitory activity on protein tyrosine phosphatase 1B (PTP1B),
compounds 〖STHZ〗2〖ST〗,〖STHZ〗4〖ST〗,〖STHZ〗9〖ST〗 have good inhibitory effects on
protein phosphatase 1 (PP1), and compounds 〖STHZ〗9〖ST〗,〖STHZ〗10〖ST〗 have a low inhibitory effect on
vaccinia H1 related (VHR) phosphatase.

Key words: Acanthopanax senticosus, active ingredient, protein , tyrosine phosphatase 1B (PTP1B), diabetes

中图分类号:

R965.1

车环宇, 赵凌志, 孙连双, 董洪坤, 滕国生. 刺五加根茎活性成分对蛋白酪氨酸磷酸酶1B的抑制作用[J]. 吉林大学学报(理学版), 2019, 57(2): 438-444.

CHE Huanyu, ZHAO Lingzhi, SUN Lianshuang, DONG Hongkun, TENG Guosheng. Inhibitory Effect of Active Ingredient from Rhizomes of Acanthopanax senticosus on Protein Tyrosine Phosphatase 1B#br#[J]. Journal of Jilin University Science Edition, 2019, 57(2): 438-444.

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