天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (5): 799-804.doi: 10.16333/j.1001-6880.2020.5.011

• 研究简报 • 上一篇    下一篇

刺五加有效成分及体外抑制二酰基甘油酰基转移酶活性研究

李志1,熊大玺2,修孟雪2,王东2,崔龙2*    

  1. 1吉林市化工医院,吉林 132101;2北华大学药学院,吉林 132013
  • 出版日期:2020-05-28 发布日期:2020-06-16
  • 基金资助:
    吉林省科技厅医药专项(20191102056YY)

Study on inhibition of diglyceride acyltransferase active components by Acanthopanax senticosus Harms

LI Zhi1,XIONG Da-xi2,XIU Meng-xue2,WANG Dong2,CUI Long2*   

  1. 1Jilin City Chemical Hospital,Jilin 132101,China;2College of Pharmacy,Beihua University,Jilin 132013,China

  • Online:2020-05-28 Published:2020-06-16

摘要:

本文为研究刺五加(Acanthopanax senticosus Harms)的化学成分及其抑制二酰基甘油酰基转移酶(DGAT)活性。刺五加用75%乙醇提取,经硅胶、ODS、半制备HPLC进行分离纯化,结合理化性质、波谱数据鉴定化合物的结构。得到12个化合物分别鉴定为赤式-愈创木基丙三醇-β-O-4′-二羟基松柏醇(1)、(E)-3-(2,2-dimethyl-2H-chromen-6-yl)prop-2-enal(2)、7′E-4,9-dihydroxy-3,3′,5′-trimethoxy-8,4′-oxyneolign-7′-en-9′-al(3)、5-甲氧基去氧双松柏醇(4)、去氧双松柏醇(5)、5,5′-二甲氧基落叶松脂素(6)、5,5′-二甲氧基开环异落叶松树脂酚(7)、(7′S,8′S)-4′-O-甲基黄花菜木脂素(8)、(+)-9′-O-(Z)-阿魏酰-5,5′-二甲氧基落叶松脂素(9)、(+)-9′-O-(E)阿魏酰-5,5′-二甲氧基落叶松脂素(10)、大豆苷(11)和3′-甲氧基大豆苷(12)。其中化合物1~3和8~10为首次从该植物中分离得到。化合物1、3~7、9和10对DGAT1活性具有抑制作用,其IC50值范围在81.5±1.2到123.2±1.1 μM之间。

关键词: 刺五加, 化学成分, 二酰基甘油酰基转移酶, 抑制剂

Abstract:

This paper studies the chemical constituents of Acanthopanax senticosus Harms and its inhibition of diacylglycerol acyltransferase (DGAT) activity.A. senticosus was extracted with 75% ethanol,and purified by silica gel,ODS and semi-preparative HPLC.The structures of the compounds were identified by physicochemical properties and spectral data.Twelve compounds were identified as erythro-guaiacylglycerol-β-O-4′-dihydroconiferyl alcohol (1),(E)-3-(2,2-dimethyl-2H-chromen-6-yl)prop-2-enal (2),7′E-4,9-dihydroxy-3,3′,5′-trimethoxy-8,4′-oxyneolign-7′-en-9′-al (3),5-methoxydehydroconiferyl alcohol (4),dehydroconiferyl alcohol (5),5,5′-dimethoxylariciresinol (6),5,5′-dimethoxysecoisolariciresinol (7),(7′S,8′S)-4′-O-methylcleomiscosin D (8),(+)-9′-O-(Z)-feruloyl-5,5′-dimethoxylariciresinol (9),(+)-9′-O-(E)-feruloyl-5,5′-dimethoxylariciresinol (10),daidzin (11) and 3′-methoxydaidzin (12),respectively.Compounds 1-3 and 8-10 were isolated from this plant for the first time.Compounds 1,3-7,9 and 10 showed inhibitory effect on DGAT1 activity with IC50 values ranging from 81.5±1.2 to 123.2±1.1 μM.

Key words: Acanthopanax senticosus Harms, chemical constituents, DGAT, inhibitor

中图分类号:  R932