中国中药杂志

2018, (23) 119-125

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夏枯草中胰脂肪酶抑制剂的筛选、鉴定与活性评价
Screening,identification and activity evaluation of pancreatic lipase inhibition in Prunella vulgaris

陈廷贵,李利亚,魏煜如,张立伟
CHEN Ting-gui,LI Li-ya,WEI Yu-ru,ZHANG Li-wei

摘要(Abstract):

该实验首先采用羧基磁珠固定化胰脂肪酶筛选出夏枯草中可能的胰脂肪酶抑制剂,然后通过LC-MS/MS鉴定,标准品比对确认,最后采用对硝基苯酚法测定抑酶活性及抑制类型。结果:从夏枯草中共筛选出4个胰脂肪酶抑制剂,并经过了LC-MS/MS鉴定和混合对照品确认,其IC_(50)和抑制类型分别为咖啡酸[(252.3±3.6) mg·L~(-1),反竞争性抑制]、芦丁[(91.2±1.6) mg·L~(-1),竞争性抑制]、橙皮苷[(31.5±4.4) mg·L~(-1),竞争性抑制]、熊果酸[(41.3±2.2) mg·L~(-1),竞争性抑制]。4抑制剂抑制类型与抑酶活性与其分子空间大小、疏水性和氢键数目,特别是与PL三联体形成氢键数目相关。
Pancreatic lipase(PL) inhibitors were firstly screened from Prunella vulgaris with PL immobilized on carboxylic acid-terminated magnetic nanoparticles, then these possible inhibitors were identified by LC-MS/MS and mixed standards. Finally, their inhibitory effects and types on PL were tested by p-nitrophenol method. The results showed that four PL inhibitors were screened out from P. vulgaris and confirmed by LC-MS/MS and mixed standards. The IC_(50) and inhibition types were as follows: caffeic acid [(252.3±3.6) mg·L~(-1), anti-competitive inhibition], rutin [(91.2±1.6)mg·L~(-1), competitive inhibition], hesperidin [(31.5±4.4) mg·L~(-1), competitive inhibition] and ursolic acid [(41.3±2.2) mg·L~(-1), competitive inhibition]. Their inhibitive types and abilities on PL were related to their molecular size, hydrophobicity and the number of hydrogen bond with PL triplet.

关键词(KeyWords): 夏枯草;固定化酶;LC-MS/MS;胰脂肪酶抑制剂
Prunella vulgaris;immobilized enzyme;LC-MS/MS;pancreatic lipase inhibitor

Abstract:

Keywords:

基金项目(Foundation): 山西省科技攻关计划项目(社会发展)(2014ZD0304)

作者(Author): 陈廷贵,李利亚,魏煜如,张立伟
CHEN Ting-gui,LI Li-ya,WEI Yu-ru,ZHANG Li-wei

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