Moraga A A, Graf U
Institute of Toxicology, Swiss Federal Institute of Technology, Schwerzenbach, Switzerland.
Mutagenesis. 1989 Mar;4(2):105-10. doi: 10.1093/mutage/4.2.105.
Nifurtimox and eight structurally related 5-nitrofuran compounds active against Trypanosoma cruzi were tested for genotoxicity in the wing somatic mutation and recombination test in Drosophila melanogaster. Nifurtimox, compound ada and compound 1B were clearly mutagenic and recombinogenic whereas the remaining six compounds were negative. In contrast to the situation in bacterial mutagenicity tests, nitroreductase activity is probably not decisive for the genotoxicity of these compounds in Drosophila. The three non-genotoxic nitrofurans with high antiparasitic activity are promising candidates for the replacement of nifurtimox. However, these compounds require further genotoxicity testing in eukaryotic assay systems for a final evaluation.
对硝呋替莫以及八种与结构相关且对克氏锥虫有活性的5-硝基呋喃化合物,在黑腹果蝇的翅体细胞突变和重组试验中进行了遗传毒性测试。硝呋替莫、化合物ada和化合物1B具有明显的致突变性和重组性,而其余六种化合物呈阴性。与细菌致突变性试验的情况不同,硝基还原酶活性可能不是这些化合物在果蝇中遗传毒性的决定性因素。三种具有高抗寄生虫活性的非遗传毒性硝基呋喃有望替代硝呋替莫。然而,这些化合物需要在真核分析系统中进行进一步的遗传毒性测试,以进行最终评估。