Lee K, Gold B, Mirvish S S
Mutat Res. 1977 Apr;48(2):131-8. doi: 10.1016/0027-5107(77)90152-x.
Twenty-two N-nitrosamides and related compounds, including 14 nitrosoureas, 5 nitrosocarbamates, and one nitrosocyanamide, were tested at various concentrations for mutagenic activity towards Salmonella typhimurium TA1535 without the use of microsomes. The ether-water partition coefficient, solubility in water, and half-life in aqueous solution were also measured. Twenty compounds were mutagenic, with "standard mutagenic concentrations" (i.e. those producing 100 mutants/dish) of 0.0024--6500 micron. Standard mutagenic concentration was negatively correlated with the partition coefficient. Three compounds (ethyl 2-acetoxyethylnitrosocarbamate, nitrosocarbaryl, and methylnitrosobenzamide) were more active than the classic mutagen methylnitrosonitroguanidine. Nitrosocarbamates were at least 50 times more mutagenic than the corresponding nitrosoureas. Nitrosodihydrouracil and propylene-nitrosourea were more active than related compounds. Ethylnitrosocyanamide was 730 times more mutagenic than ethylnitrosourea. Fifteen of the test compounds (of which 14 were mutagenic) had previously been assayed in rats for carcinogenicity, all with positive results.
在不使用微粒体的情况下，对22种N-亚硝基酰胺及相关化合物进行了测试，其中包括14种亚硝基脲、5种亚硝基氨基甲酸酯和1种亚硝基氰胺，测试了它们在不同浓度下对鼠伤寒沙门氏菌TA1535的致突变活性。还测量了它们的醚-水分配系数、在水中的溶解度以及在水溶液中的半衰期。20种化合物具有致突变性，“标准致突变浓度”（即每皿产生100个突变体的浓度）为0.0024 - 6500微米。标准致突变浓度与分配系数呈负相关。三种化合物（2-乙酰氧基乙基亚硝基氨基甲酸乙酯、亚硝基西维因和亚硝基苯甲酰胺）比经典诱变剂甲基亚硝基胍更具活性。亚硝基氨基甲酸酯的致突变性至少是相应亚硝基脲的50倍。亚硝基二氢尿嘧啶和亚硝基丙烯脲比相关化合物更具活性。亚硝基氰胺的致突变性是亚硝基脲的730倍。15种受试化合物（其中14种具有致突变性）此前已在大鼠中进行致癌性测定，结果均为阳性。
