Heinemann B
Appl Microbiol. 1972 Jan;23(1):91-7. doi: 10.1128/am.23.1.91-97.1972.
Prophage induction in lysogenic Escherichia coli W1709 (iota) was determined for 29 N-nitroso compounds, 13 of their denitrosated derivatives, and 7 hydroxylamino and hydrazino analogues of nitrosamines. Minimal inducing concentrations of 0.1 to 2.0 mug/ml were demonstrated for eight nitrosamidines, and concentrations of 0.5 to 25.0 mug/ml were shown for six nitrosamides. Weak inducing activities were found with N,N-diethylhydroxylamine oxalate and N-methyl-N-phenylhydrazine sulfate, derivatives of inactive N-nitrosodiethylamine and N-nitrosomethylphenylamine, respectively. Inactive compounds including N-methyl-N-nitroso-p-toluenesulfonamide, 11 nitrosamines, 3 N, N'-dialkyl substituted-N-nitrosoureas, 13 denitrosated derivatives, and 5 hydroxylamino and hydrazino analogues of nitrosamines are listed. Since 7 of the 14 prophage-inducing nitrosamidines and nitrosamides reported thus far have carcinostatic activity in rodent tumor systems, it is concluded that the induction test may provide a useful screen for the detection of potential antitumor compounds. The induction test may also be useful for the detection of responsive N-nitroso compounds which may be potential toxicological hazards in the environment since, of the six active nitrosamides, five have already been reported to produce mutagenic and carcinogenic effects, four produce chromosomedamaging effects, and two produce teratogenic effects. Use of the prophage induction system for detection of biologically active intermediates formed by N-nitroso compounds under physiological conditions is considered.
测定了29种N-亚硝基化合物、13种其脱亚硝基衍生物以及7种亚硝胺的羟氨基和肼基类似物对溶源性大肠杆菌W1709(iota)的前噬菌体诱导作用。8种亚硝基脒的最小诱导浓度为0.1至2.0微克/毫升,6种亚硝酰胺的诱导浓度为0.5至25.0微克/毫升。分别发现草酸N,N-二乙羟胺和硫酸N-甲基-N-苯基肼有较弱的诱导活性,它们分别是无活性的N-亚硝基二乙胺和N-亚硝基甲基苯胺的衍生物。列出了无活性的化合物,包括N-甲基-N-亚硝基对甲苯磺酰胺、11种亚硝胺、3种N,N'-二烷基取代的N-亚硝基脲、13种脱亚硝基衍生物以及5种亚硝胺的羟氨基和肼基类似物。由于迄今为止报道的14种能诱导前噬菌体的亚硝基脒和亚硝酰胺中有7种在啮齿动物肿瘤系统中具有抗癌活性,因此得出结论,诱导试验可为检测潜在的抗肿瘤化合物提供有用的筛选方法。诱导试验对于检测可能在环境中具有潜在毒理学危害的反应性N-亚硝基化合物也可能有用,因为在6种有活性的亚硝酰胺中,已有5种被报道会产生诱变和致癌作用,4种会产生染色体损伤作用,2种会产生致畸作用。考虑使用前噬菌体诱导系统检测N-亚硝基化合物在生理条件下形成的生物活性中间体。