journal6 ›› 2012, Vol. 33 ›› Issue (6): 85-88.DOI: 10.3969/j.issn.1007-2985.2012.06.020

• 化学化工 • 上一篇    下一篇

4-(4-羟基苯基)乙基儿茶酚作为尿素酶抑制剂的机理

  

  1. (吉首大学化学化工学院,湖南 吉首 416000)
  • 出版日期:2012-11-25 发布日期:2013-01-14
  • 通讯作者: 肖竹平(1972-),湖南邵阳人,吉首大学化学化工学院副教授,博士,主要从事药物化学和应用有机化学;E-mail:xiaozhuping2005@163.com.
  • 作者简介:彭知云(1986-),湖南邵阳人,硕士,主要从事药物化学和应用有机化学研究
  • 基金资助:

    国家自然科学基金资助项目(81273382);湖南省自然科学基金资助项目(11JJ3113);吉首大学校级科研资助项目(11JDY048)

Study on the Inhibition Mechanism of 4-(4-Hydroxyphenethyl)Benzene-1,2-Diol on Urease

  1. (College of Chemistry and Chemical Engineering,Jishou University,Jishou 416000,Hunan China)
  • Online:2012-11-25 Published:2013-01-14

摘要:4-(4-羟基苯基)乙基儿茶酚是一种新型幽门螺旋杆菌尿素酶抑制剂,运用酶动力学研究方法,对它的抑制机理、抑制类型进行探讨.实验结果表明,4-(4-羟基苯基)乙基儿茶酚是尿素酶的竞争性抑制剂,抑制常数Ki为1.48 μmol/L,为其在抗胃炎、胃溃疡方面的应用以及进一步的结构优化奠定了理论基础.

关键词: 幽门螺旋杆菌尿素酶, 4-(4-羟基苯基)乙基儿茶酚, 酶动力学, 竞争性抑制

Abstract: 4-(4-Hydroxyphenethyl)benzene-1,2-diol is a new inhibitor against Helicobacter Pylori urease.The inhibition mechanism was herein investigated through enzyme kinetics methods,and the results revealed that 4-(4-hydroxyphenethyl)benzene-1,2-diol was competitive inhibitor of urease with a Ki value of 1.48 μmol/L.The chemical stabilitiy and the competitive mechanism of 4-(4-hydroxyphenethyl)-benzene-1,2-diol strongly suggested that it could be used as a lead compound for rational drug design to find active compound and as a potential urease inhibitor for treatment of gastritis and peptic ulcer.

Key words: Helicobacter Pylori urease, 4-(4-hydroxyphenethyl)benzene-1,2-diol, enzyme kinetics, competitive inhibition

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