King C L, Wong S K, Loo T L
Eur J Cancer Clin Oncol. 1984 Feb;20(2):261-4. doi: 10.1016/0277-5379(84)90193-7.
The bifunctional cross-linking activity of 3,6-diaziridinyl-2,5-bis(carboethoxyamino)-1,4-benzoquinone (AZQ, NSC 182986) on isolated calf thymus DNA was studied, using ethidium bromide fluorescence assay. Between 1 and 350 microM AZQ produced a dose-dependent cross-linking effect in the presence of a 10-fold excess of sodium borohydride. No cross-linking was observed in the absence of the reducing agent. AZQ can also be activated by NADH and NADPH at pH 4. The AZQ cross-linking activity exhibited a strong pH dependency, highest at acidic pH, lower at alkaline pH and not seen under neutral conditions. It was also significantly inhibited under anaerobic conditions. At pH 5 the binding ratio was 1 molecule of AZQ per 191 bases at an AZQ dose of 300 microM. Our results suggest that reduced AZQ behaved like a bifunctional alkylating agent.
利用溴化乙锭荧光分析法，研究了3,6 - 二氮丙啶基 - 2,5 - 双（乙氧羰基氨基）- 1,4 - 苯醌（AZQ，NSC 182986）对分离的小牛胸腺DNA的双功能交联活性。在存在10倍过量硼氢化钠的情况下，1至350微摩尔的AZQ产生了剂量依赖性的交联效应。在没有还原剂的情况下未观察到交联现象。在pH 4时，AZQ也可被NADH和NADPH激活。AZQ交联活性表现出强烈的pH依赖性，在酸性pH下最高，在碱性pH下较低，在中性条件下则未观察到。在厌氧条件下也受到显著抑制。在pH 5时，在300微摩尔的AZQ剂量下，结合比例为每191个碱基1个AZQ分子。我们的结果表明，还原态的AZQ表现得像一种双功能烷基化剂。
