摘要
从牛蒡子、胡黄连中筛选对猪磷酸二酯酶(PDE)7A2具有抑制作用的中药单体成分,为PDE亚型抑制剂研究积累资料。使用高效液相色谱法(HPLC)测定绿原酸、牛蒡子苷、β-谷甾醇和胡黄连苷-Ⅱ对体外原核表达的猪PDE7A2的抑制作用。结果表明:在反应质量浓度为1,5,10,50,100μmol/L时,绿原酸对猪PDE7A2的活性抑制率分别为12.55%,46.29%,56.17%,68.52%,47.12%;牛蒡子苷抑制率分别为21.60%,41.35%,70.16%,88.27%,80.07%;β-谷甾醇抑制率分别为40.53%,54.52%,71.81%,96.50%,94.86%;胡黄连苷-Ⅱ抑制率分别为69.34%,94.03%,96.50%,103.09%,101.44%。绿原酸、牛蒡子苷、β-谷甾醇和胡黄连苷-Ⅱ对体外表达的猪PDE7A2均有抑制作用,其中胡黄连苷-Ⅱ对猪PDE7A2的抑制作用最强。
[Purpose] The aims of this paper were to screen the monomers of Chinese traditional herbs Fructus Arctii and Picrorhiza which could inhibit Porcine PDE7A2 activity.[Methods] The inhibiting effects of chlorogenic acid,arctiin which the effictive component of Picrorhiza and β sitosterol,picroside Ⅱ which the effictive component of Fructus Arctii on in vitro prokaryotic expressed Porcine PDE7A2 were determined by High Performance Liquid Chromatography （HPLC）.[Results] With the reaction concentrations of 1μmol/L,5μmol/L,10μmol/L,50μmol/L and 100μmol/L,the activity inhibiting ratios of chlorogenic acidare 12.55％,46.29％,56.17％,68.52％ and 47.12％ respectively; those of arctiin are 21.60％,41.35％,70.16％,88.27％ and 80.07％ respectively; those of β sitosterol are 40.53％,54.52％,71.81％,96.50％ and 94.86％ respectively,and those of picroside Ⅱ are 69.34％,94.03％,96.50％,103.09％ and 101.44％ respectively.[Conclusion] Chlorogenic acid,arctiin,β sitosterol and picroside Ⅱ all had inhibiting effects on Porcine PDE7A2 in vitro prokaryotic expression,among which picroside Ⅱ had strongest inhibiting function.
出处
《北京农学院学报》
2014年第4期65-68,共4页
Journal of Beijing University of Agriculture
基金
北京市属高等学校人才强教计划资助项目资助(PHR201107134)
北京市自然科学基金资助项目(6112007)
关键词
猪
磷酸二酯酶7A2
胡黄连
牛蒡子
porcine
phosphodiesterase 7A2
fructus arctii
picrorhiza
