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

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

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±1.1μM之间。

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±1.1μM.