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  • 标题:ニコチン酸アミドを用いる各種アルキル化剤のアルキル化能測定について
  • 本地全文:下载
  • 作者:平山 晃久 ; 宇田 和彦 ; 小野 晴美
  • 期刊名称:Journal of Health Science
  • 印刷版ISSN:1344-9702
  • 电子版ISSN:1347-5207
  • 出版年度:1988
  • 卷号:34
  • 期号:2
  • 页码:152-155
  • DOI:10.1248/jhs1956.34.152
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Alkylating activities of various alkylating agents were examined by using nicotinamide. One μmol of alkylating agent was incubated with nicotinamide (25-200 μmol) in a phosphate buffer (pH 7.4) at 37°C for 24 h. The resulting N1-alkylnicotinamide was converted to 2-alkyl-6-phenyl-2, 8-dihydro-8-oxo-2, 7-naphthyridine and analyzed by high-performance liquid chromatography with a fluorescent detector. Alkylating activity was expressed as percentage of the formed N1-alkylnicotinamide against 1 μmol of the standard N1-alkylnicotinamide. In methylation and ethylation, the alkylating activity was in the order of methyl methanesulfonate (100%), dimethyl sulfate (68%), methyl iodide (21%) and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG) (20%), and ethyl methanesulfonate (93%), diethyl sulfate (68%), ethyl iodide (3%) on addition of 200 μmol nicotinamide. MNNG known as mutagen and carcinogen, have not so high activity. Propylene oxide and 1, 2-butylene oxide show 100% alkylating activities under the same reaction conditions as described above on addition of 200 μmol nicotinamide.
  • 关键词:Alkylating agent;Alkylating activity;Nicotinamide;N1-Alkylnicotinamide;HPLC
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