Baguley B C, Ferguson L R, Denny W A
Chem Biol Interact. 1982 Oct;42(1):97-105. doi: 10.1016/0009-2797(82)90145-4.
Proflavine (3,6-diaminoacridine) and its 2,7-dimethyl, 2,7-diethyl, 2,7-diisopropyl and 2,7 di-t-butyl derivatives have been compared with respect to their DNA binding and biological properties. The binding of the first three members of the series to covalently closed circular duplex DNA showed the unwinding properties expected of intercalators. The 2,7-diisopropyl showed intermediate properties and the 2,7-di-t-butyl derivative failed to unwind this DNA. Antibacterial toxicity, measured in cultures of Salmonella typhimurium, increased with increasing lipophilic character of the compounds. Mutagenicity in the TA1537 frameshift tester strain was restricted to the first two members of the series, although the mutagenicity of the more lipophilic members may have been masked by toxicity. In contrast, toxicity towards cultures of L1210 cells showed a possible transition between intercalating and non-intercalating derivatives. It is proposed that DNA intercalation provides the major component of the toxicity towards cultured leukaemia cells, whereas lipophilicity provides the major component towards bacteria.
已对硫酸普罗黄素（3,6 - 二氨基吖啶）及其2,7 - 二甲基、2,7 - 二乙基、2,7 - 二异丙基和2,7 - 二叔丁基衍生物的DNA结合特性和生物学特性进行了比较。该系列的前三个成员与共价闭合环状双链DNA的结合显示出嵌入剂预期的解旋特性。2,7 - 二异丙基衍生物表现出中间特性，而2,7 - 二叔丁基衍生物未能使这种DNA解旋。在鼠伤寒沙门氏菌培养物中测得的抗菌毒性随着化合物亲脂性的增加而增加。在TA1537移码测试菌株中的诱变性仅限于该系列的前两个成员，尽管亲脂性更强的成员的诱变性可能已被毒性掩盖。相比之下，对L1210细胞培养物的毒性显示出嵌入和非嵌入衍生物之间可能的转变。有人提出，DNA嵌入是对培养的白血病细胞毒性的主要组成部分，而亲脂性是对细菌毒性的主要组成部分。
