Enhancement of Mutagenic Activity of 9-Aminoacridine by Introducing a Nitro Group into the Molecule
作者:Hideyuki Tomosaka、Saburo Omata、Kentaro Anzai
DOI:10.1271/bbb.58.1420
日期:1994.1
Mutagenic activity and DNA intercalation were examined for 9-aminoacridine (9-AA) and its derivatives. Introduction of a nitro group into the 9-AA molecule was found to enhance the activity enormously as was detected by the Ames test. Acetylation of amino group at 9-position of acridine ring inhibited the intercalation, the frameshift activity disappearing. Rat liver S9 converted 9-AA metabolically to 9-amino-2-hydroxyacridine.
对9-氨基嘧啶(9-AA)及其衍生物进行了突变活性和DNA夹杂作用的研究。向9-AA分子中引入硝基基团被发现显著增强了活性,这在Ames测试中得到了验证。对嘧啶环上9位氨基的乙酰化抑制了夹杂作用,移码活性消失。大鼠肝脏S9将9-AA转化为9-氨基-2-羟基嘧啶。