INHIBITION OF P-450 BY AUCUBIN - IS THE BIOLOGICAL-ACTIVITY OF AUCUBIN DUE TO ITS GLUTARALDEHYDE-LIKE AGLYCONE

被引：36

作者：

BARTHOLOMAEUS, A

AHOKAS, J

机构：

[1] Key Centre for Applied and Nutritional Toxicology, RMIT, Melbourne

来源：

TOXICOLOGY LETTERS | 1995年 / 80卷 / 1-3期

关键词：

CARBON TETRACHLORIDE; GLUTARALDEHYDE; AUCUBIN; IRIDOID; HEPATOTOXICITY;

D O I：

10.1016/0378-4274(95)03339-M

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

The inhibition of ethoxy coumarin O-deethylase (ECOD)activity By aucubin and its aglycone was examined in a microsomal system and in freshly isolated hepatocytes. Aucubin was found to be inactive but the aglycone was found to be a potent time-dependent inhibitor of ECOD activity in both systems. The close structural similarity between the aglycone of aucubin and glutaraldehyde suggests a similiar mechanism of enzyme inhibition through protein cross-linking by Schiff reactions. The similarity between the 2 compounds was demonstrated through their closely similar binding spectra to bovine serum albumin. The biological activities reported for the aglycone are suggested to be due to this similarity tb glutaraldehyde.

引用

页码：75 / 83

页数：9

共 17 条

[1] A CRITICAL-REVIEW OF THE TOXICOLOGY OF GLUTARALDEHYDE [J].