文章基本信息

标题：Dihydropyrazine Derivatives as a New Type of DNA Strand Breaking Agent
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作者：Tadatoshi YAMAGUCHI ; Nobuhiro KASHIGE ; Noriko MISHIRO 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1996
卷号：19
期号：10
页码：1261-1265
DOI：10.1248/bpb.19.1261
出版社：The Pharmaceutical Society of Japan
摘要：The DNA strand-breaking activity of some dihydropyrazine derivatives, 2, 3-dihydro-5, 6-dimethylpyrazine (3), 2, 3-dihydro-2, 5, 6-trimethylpyrazine (4), 2, 3-dihydro-2, 2, 5, 6-tetramethylpyrazine (5), trans-2, 3-dimethyl-5, 6, 7, 8, 9, 10-hexahydroquinoxaline (6), its cis-compound (7) and the mixture of 6 and 7 (8) was tested by agarose gel electrophoresis using plasmide pBR322 ccc-DNA as a substrate. The order of DNA strand-breaking activity in the presence of Cu²⁺ was (7)>(8)≥(5)>(2)>(6)>(4)≥(1)≥(3). 2, 5-Bis(D-arabino-tetrahydroxybutyl)-2, 5-dihydropyrazine (1) and 2, 5-dihydro-3, 6-dimethylpyrazine (2) have already been described in terms of DNA breaking activity in a previous paper.The activity was suggested to be due to the dihydropyrazine skeleton, in addition to active oxygen radicals formed in an aqueous solutoin. The introduction of a methyl group to the dihydropyrazine skeleton enhanced the activities of dihydropyrazine derivatives. The possible chemical basis for DNA strand breakage by dihydropyrazine derivatives, especially in the presence of Cu²⁺, was discussed.
关键词：dihydropyrazine;DNA strand-breaking activity;plasmid pBR322;radical ion;cupric ion