Ozawa S, Nagata K, Yamazoe Y, Kato R
Department of Pharmacology, School of Medicine, Keio University, Tokyo.
Jpn J Cancer Res. 1995 Mar;86(3):264-9. doi: 10.1111/j.1349-7006.1995.tb03049.x.
In rat liver cytosol systems, 2-amino-3-methylimidazo[4,5-f]quinoline (IQ) and 2-amino-3,8-dimethylimidazo[4,5-f]quinoxaline (MeIQx) were converted into their sulfamates in the presence of 3'-phosphoadenosine 5'-phosphosulfate at rates of 51.2 and 50.7 pmol/min/mg cytosol in the male, and 23.7 and 22.5 pmol/min/mg cytosol in the female, respectively. IQ-sulfamate formation was low (0.24 pmol/min/mg cytosol) in human liver cytosols, and MeIQx-sulfamate was not detected (< 0.1 pmol/min/mg cytosol). These results suggest only a minor contribution of IQ- and MeIQx-sulfamate formation to the detoxification of both heterocyclic amines in humans. Using sulfotransferase cDNA-expression systems, a rat ST1A1 arylsulfotransferase has been shown to catalyze the formation of the sulfamates, suggesting a role of the ST1A type of sulfotransferase in the N-sulfation of heterocyclic amines.
在大鼠肝脏胞质溶胶系统中,在3'-磷酸腺苷5'-磷酸硫酸酯存在的情况下,2-氨基-3-甲基咪唑并[4,5-f]喹啉(IQ)和2-氨基-3,8-二甲基咪唑并[4,5-f]喹喔啉(MeIQx)分别以雄性51.2和50.7皮摩尔/分钟/毫克胞质溶胶、雌性23.7和22.5皮摩尔/分钟/毫克胞质溶胶的速率转化为它们的氨基磺酸酯。在人肝脏胞质溶胶中,IQ-氨基磺酸酯的形成较低(0.24皮摩尔/分钟/毫克胞质溶胶),且未检测到MeIQx-氨基磺酸酯(<0.1皮摩尔/分钟/毫克胞质溶胶)。这些结果表明,IQ-和MeIQx-氨基磺酸酯的形成对人体中这两种杂环胺解毒的贡献较小。利用磺基转移酶cDNA表达系统,已证明大鼠ST1A1芳基磺基转移酶可催化氨基磺酸酯的形成,这表明ST1A类型的磺基转移酶在杂环胺的N-硫酸化中发挥作用。