Inhibition of porcine liver carboxylesterase by a new flavone glucoside isolated from Deverra scoparia
Inhibition of porcine liver carboxylesterase by a new flavone glucoside isolated from Deverra scoparia
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DOI：
10.1016/j.cbi.2007.11.008
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发表时间：
2008-03-10
影响因子：
5.1
通讯作者：
Stocker, P.
中科院分区：
文献类型：
--
作者：
Djeridane, A.;Brunel, J. M.;Stocker, P.
一种来自伞形科的北非撒哈拉特有植物，Deverra scoparia，在当地用于药物制剂，对猪肝羧酸酯酶表现出强烈的抑制作用。通过半制备HPLC和光电二极管阵列检测从植物的地上部分的活性化合物进行纯化，并通过H-1，C-13 NMR和质谱方法确定结构。该化合物经鉴定为黄酮-3，4 ′，7-三羟基-3 ′-甲氧基-7-葡萄糖苷，是猪肝羧酸酯酶的强竞争性抑制剂，抑制常数为16 μ M。基于抑制剂和酶活性位点区域的结构特征，似乎黄酮苷结合到酶的表面。低Ki值表明这种抑制活性的某些生理意义，特别是关于异生物质的生物转化。(C)2007爱思唯尔爱尔兰有限公司保留所有权利。
An endemic North African Saharan plant from of the Apiaceae family, Deverra scoparia, used locally for medicinal preparations, showed a strong inhibitory effect on porcine liver carboxylesterase. The active compound from the aerial part of the plant was purified by semi-preparative HPLC and photodiode array detection, and structurally determined by H-1, C-13 NMR and mass spectroscopy methods. This compound was identified as flavone-3,4',7-trihydroxy-3'-methoxy-7-glucoside and it was found to be a powerful competitive inhibitor of porcine liver carboxylesterase with a inhibition constant value of 16 mu M. Based on the structural features of the inhibitor and the enzyme active site region, it seems that the flavonoside binds to the surface of the enzyme. The low K-i value suggests some physiological significance of such inhibitory activity, especially concerning the bio-transformation of xenobiotics. (C) 2007 Elsevier Ireland Ltd. All rights reserved.