Guengerich F P, Peterson L A, Cmarik J L, Koga N, Inskeep P B
Department of Biochemistry, Vanderbilt University School of Medicine, Nashville, TN 37232.
Environ Health Perspect. 1987 Dec;76:15-8. doi: 10.1289/ehp.877615.
Ethylene dibromide (1,2-dibromoethane, EDB) can be activated to electrophilic species by either oxidative metabolism or conjugation with glutathione. Although conjugation is generally a route of detoxication, in this case it leads to genetic damage. The major DNA adduct has been identified as S-[2-(N7-guanyl)ethyl]glutathione, which is believed to arise via half-mustard and episulfonium ion intermediates. The adduct has a half-life of about 70 to 100 hr and does not appear to migrate to other DNA sites. Glutathione-dependent DNA damage by EDB was also demonstrated in human hepatocyte preparations. The possible relevance of this DNA adduct to genetic damage is discussed.
二溴乙烷（1,2 - 二溴乙烷，EDB）可通过氧化代谢或与谷胱甘肽结合被激活为亲电物质。虽然结合通常是一种解毒途径，但在这种情况下它会导致基因损伤。主要的DNA加合物已被鉴定为S - [2 - （N7 - 鸟嘌呤基）乙基]谷胱甘肽，据信它是通过半芥子气和环锍离子中间体产生的。该加合物的半衰期约为70至100小时，似乎不会迁移到其他DNA位点。在人肝细胞制剂中也证实了EDB依赖谷胱甘肽的DNA损伤。讨论了这种DNA加合物与基因损伤的可能相关性。
