Comparative misonidazole metabolism in anaerobic bacteria and hypoxic Chinese hamster lung fibroblast (V-79-473) cells.
Comparative misonidazole metabolism in anaerobic bacteria and hypoxic Chinese hamster lung fibroblast (V-79-473) cells.
复制标题
厌氧菌和缺氧中国仓鼠肺成纤维细胞 (V-79-473) 细胞中米索硝唑代谢的比较。
DOI：
10.1016/0006-2952(82)90190-3
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发表时间：
1982
影响因子：
5.8
通讯作者：
Goldman,P
中科院分区：
文献类型：
--
作者：
Koch,RL;Rose,C;Rich,TA;Goldman,P
辐射增敏剂米索硝唑在无氧盲肠内容物和缺氧中国仓鼠肺成纤维细胞（V-79-473）中的代谢相似。这两种体系都形成了咪唑的氨基衍生物[1-（2-氨基咪唑-1-基）-3-甲氧基丙烷-2-醇]（AIM）和尿素，以及代谢物（2-羟基-3-甲氧基丙基）-胍(G)，这在以前没有被描述过。米索硝唑的硝基似乎被还原成AIM，然后该化合物被水解生成尿素或G，后者的产量为25%（组织培养）至55%（盲肠内容物）。当用Ames测试菌株进行测试时，G和AIM仅对菌株ta98具有轻微的致突变性，并且仅在微粒体激活系统存在时才具有致突变性。
The metabolism of the radiation sensitizer misonidazole was similar in anaerobic cecal contents and hypoxic Chinese hamster lung fibroblasts (V-79-473). Both systems formed the amino derivative of misonidazole, [1-(2-aminoimidazol-1-yl)-3-methoxypropan-2-ol] (AIM), and urea, as well as a metabolite, (2-hydroxy-3-methoxypropyl)-guanidine (G), which has not been described previously. It appears that the nitro group of misonidazole was reduced to form AIM and that this compound was then hydrolyzed to yield either urea or G, the latter in yields of 25% (tissue culture) to 55% (cecal contents). When tested with the Ames tester strain, both G and AIM were slightly mutagenic only for strain TA 98 and then only in the presence of the system for microsomal activation.