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

概要

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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℃ for 24 h. The resulting N^1-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 N^1-alkylnicotinamide against 1 μmol of the standard N^1-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.
公益社団法人日本薬学会の論文
1988-04-30