O'Sullivan M C, Dalrymple D M, Zhou Q
Department of Chemistry, Indiana State University, Terre Haute 47809, USA.
J Enzyme Inhib. 1996 Oct;11(2):97-114. doi: 10.3109/14756369609036537.
Trypanothione reductase is a vital component of the antioxidant defenses of trypanosomes. This enzyme reduces trypanothione, a spermidine-glutathione conjugate. The inhibitory effects of several spermidine derivatives on the reduction of trypanothione by Trypanosoma cruzi trypanothione reductase were assessed. Spermidine derivatives containing hydrophobic aromatic substituents were found to be competitive inhibitors of trypanothione reductase. N4-acylated spermidine derivatives were less effective inhibitors than the corresponding N4-alkylated derivatives. The most effective compounds studied were N1, N8-bis(2-naphthylmethyl)spermidine and N4-(2-naphthylmethyl)spermidine, with Ki values of 9.5 and 108 microM, respectively.
锥虫硫醇还原酶是锥虫抗氧化防御系统的重要组成部分。该酶可还原锥虫硫醇，一种亚精胺 - 谷胱甘肽共轭物。评估了几种亚精胺衍生物对克氏锥虫锥虫硫醇还原酶还原锥虫硫醇的抑制作用。发现含有疏水芳香取代基的亚精胺衍生物是锥虫硫醇还原酶的竞争性抑制剂。N4 - 酰化亚精胺衍生物的抑制效果不如相应的N4 - 烷基化衍生物。所研究的最有效化合物是N1, N8 - 双(2 - 萘甲基)亚精胺和N4 - (2 - 萘甲基)亚精胺，其Ki值分别为9.5和1〇8微摩尔。 （注：原文中“108 microM”推测应为“108 μM”，译文按修正后翻译）
