高等学校化学学报

高等学校化学学报 ›› 2012, Vol. 33 ›› Issue (12): 2692.doi: 10.7503/cjcu20120436S

• 有机化学 • 上一篇    下一篇

磁珠富集与液相色谱-质谱联用结合筛选枳壳中脂肪酶抑制剂

陈锥1, 陶益1, 王怡2, 王毅1   

  1. 1. 浙江大学药物信息研究所, 杭州 310058;
    2. 天津中医药大学中医药研究院, 天津 300193
  • 收稿日期:2012-05-04 出版日期:2012-12-10 发布日期:2012-11-20
  • 通讯作者: 王毅,男,博士,副教授,主要从事中药药效物质快速发现技术方面的研究.E-mail:mysky@zju.edu.cn E-mail:mysky@zju.edu.cn
  • 基金资助:

    国家"重大新药创制"科技重大专项课题(批准号: 2012ZX09304-007)和国际科技合作项目(批准号: 2009DFB30510)资助.

Rapid Screening of Lipase Inhibitors from Fructus aurantii Using Lipase-immobilized Magnetic Beads Coupled with High-performance Liquid Chromatography-Mass Spectrometry

CHEN Zhui1, TAO Yi1, WANG Yi2, WANG Yi1   

  1. 1. Pharmaceutical Informatics Institute, Zhejiang University, Hangzhou 310058, China;
    2. Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
  • Received:2012-05-04 Online:2012-12-10 Published:2012-11-20

PDF (PC)

被引次数

13

摘要：

提出了一种磁珠收集与液相色谱-质谱联用(LC-MS)结合用于快速筛选中药提取物中的脂肪酶抑制剂的方法. 通过制备键合脂肪酶的磁珠, 将其与枳壳总黄酮孵育后, 筛选出枳壳中脂肪酶的配体. 通过LC-MS分析发现, 4个化合物均是潜在的脂肪酶抑制剂, 鉴定其分别为柚皮苷、 新橙皮苷、 橙皮苷和枸橘苷. 对4个化合物进行了体外脂肪酶抑制活性验证. 研究结果表明, 新橙皮苷、 橙皮苷和枸橘苷具有显著的脂肪酶抑制活性, IC50分别为48.04, 52.45和46.18 μg/mL, 其中枸橘苷具有脂肪酶抑制活性为首次报道. 结果表明, 磁珠富集与LC-MS集成技术能够用于快速发现中药活性成分.

关键词: 脂肪酶, 磁珠富集, 枳壳, 配体筛选

Abstract:

A new method for the rapidly screening of lipase inhibitors from extracts of traditional Chinese medicine using lipase-immobilized magnetic beads coupled with high-performance liquid chromatography-mass spectrometry(LC-MS) was proposed. After the lipase-immobilized magnetic beads were prepared, they were incubated with total flavonoid of Fructus aurantii to fish the ligands of lipase. Then, the eluent of magnetic beads' screening was analyzed by LC-MS. Four compounds, as naringin, hesperidin, neohesperidin and poncirin, were identified as the potential lipase inhibitors. Furthermore, the in vitro inhibitory activities against lipase of four compounds were tested. The results showed that hesperidin, neohesperidin and poncirin exhibit lipase inhibitory activities, while poncirin was firstly reported to be a lipase inhibitor. Our research showed that active compounds could be rapidly screened from extracts of traditional Chinese medicine via lipase-immobilized magnetic beads coupled with LC-MS.

Key words: Lipase, Magnetic beads' screening, Fructus aurantii, Ligand fishing

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