椭圆叶贯叶金丝桃中的脲酶抑制剂

Urease inhibitors from Hypericum oblongifolium WALL.

机构信息

Institute of Chemical Sciences, University of Peshawar, Peshawar, Pakistan.

出版信息

J Enzyme Inhib Med Chem. 2010 Apr;25(2):296-9. doi: 10.3109/14756360903179385.

PMID:20222765

Abstract

The bioassay-guided fractionation of H. oblongifolium has led to the isolation of potent urease inhibitors 1-3. The structures were elucidated by NMR and mass spectroscopic techniques. Compound 2 showed a potent enzyme inhibition activity (IC(50) 20.96 +/- 0.93), which is comparatively higher than that for the standard thiourea (IC(50) 21.01 +/- 0.51 microM). Compounds 1 and 3 also showed a significant activity, with IC(50) 37.95 +/- 1.93 and 138.43 +/- 1.23 microM, respectively. The sub crude fractions (F1, F2, F3, and F4) were tested in vitro for their urease inhibition activity. Fractions F2 and F4 showed significant activity with IC(50) 140.37 +/- 1.93 and 167.43 +/- 3.03 microM, respectively.

摘要

经过生物活性导向分离，从长叶胡颓子中分离得到了具有强抑制脲酶活性的化合物 1-3。通过 NMR 和质谱技术解析了化合物的结构。化合物 2 表现出很强的酶抑制活性（IC50 为 20.96 +/- 0.93），比标准试剂硫脲（IC50 为 21.01 +/- 0.51 microM）高。化合物 1 和 3 也具有显著的活性，IC50 分别为 37.95 +/- 1.93 和 138.43 +/- 1.23 microM。对粗提物的各个部分（F1、F2、F3 和 F4）进行了体外脲酶抑制活性测试。F2 和 F4 部分显示出显著的活性，IC50 分别为 140.37 +/- 1.93 和 167.43 +/- 3.03 microM。