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  • 标题:2,4-Dinitrobiphenyl誘導体の変異原性代謝物質の構造について
  • 本地全文:下载
  • 作者:平山 晃久 ; 井口 和彦 ; 山中 幸義
  • 期刊名称:Journal of Health Science
  • 印刷版ISSN:1344-9702
  • 电子版ISSN:1347-5207
  • 出版年度:1991
  • 卷号:37
  • 期号:3
  • 页码:229-238
  • DOI:10.1248/jhs1956.37.229
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:In order to elucidate the mechanisms of mutagenic activation of nitrobiphenyls in Salmonella typhimurium TA98 by use of a mammalian activation system, 2, 4, 6-trinitrobiphenyl (TNBp, 0.09 rev./nmol+S9) and 2, 4, 2', 4'-tetranitrobiphenyl (TNBp*, 457.19 rev./nmol+S9) were incubated with 10% S9 mix, separately, and their mutagenic metabolites were separated by SiO2 and Al2O3 column chromatography. In 2, 4, 6-TNBp, 4-amino-2, 6-dinitroBp (0.11 rev./nmol-S9) and 2, 4-diamino-6-nitroBp (0.50 rev./nmol-S9) were isolated from the reaction mixture of TNBp with S9 mix at 37°C for 48 h, and their structures determined by their mass and 1H-NMR spectra and the GC/MS data of their deamination products. In 2, 4, 2', 4'-TNBp*, 2, 4'-diamino-2', 4-dinitroBp (25460.01 rev./nmol-S9) and 2, 2'-dinitrobenzidine (33.79 rev./nmol-S9) were isolated from the reaction mixture, and their structures also determined by their physico-chemical and the GC/MS data of their deamination products. From the high-performance liquid chromatographic analysis of these metabolites, the mutagenicity of 2, 4'-diamino-2', 4-dinitroBp (-S9) contributed 100% of the mutagenicity of 2, 4, 2', 4'-TNBp* (+S9), whereas the mutagenicity of 4-amino-2, 6-dinitroBp and 2, 4-diamino-6-nitroBp contributed only 0.8 and 0.4% of that of 2, 4, 6-TNBp (+S9), respectively. Mutagenicity of 2, 2'-dinitrobenzidine was reduced to a half by the treatment with S9 mix, whereas the mutagenicity was expected to be enhanced by a mammalian metabolic activation system.
  • 关键词:mutagenicity;Salmonella typhimurium TA98;2, 4-dinitrobiphenyl derivatives;2, 4, 6-trinitrobiphenyl;2, 4, 2', 4'-tetranitrobiphenyl;mammalian metabolic activation system (S9 mix);2, 4'-diamino-2', 4-dinitrobiphenyl
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