Nemoto N, Hirakawa T, Takayama S
Chem Biol Interact. 1978 Jul;22(1):1-14. doi: 10.1016/0009-2797(78)90145-x.
The formation of water-soluble metabolites of tritium-labeled benzo[a]pyrene (BP) by cultured hamster embryo cells was studied. The ratio of the radioactivity in the aqueous phase to that in the organic phase increased with the incubation period. After incubation for 48 h with 3.75 nmol/ml of [3H] BP in the medium more than 90% of the 3H-radioactivity was found in the aqueous phase, whereas with 10-fold more BP about half the radioactivity remained in the organic phase. The main metabolites extracted from the medium at 37.5 nmol/ml BP with ethyl acetate by high pressure liquid chromatography (HPLC) were 9,10-diol and 7,8-diol; but after treatment of the medium with beta-glucuronidase the main oxygenated metabolites were phenols, the amount of 9-OH BP being more than that of 3-OH BP. beta-Glucuronidase also released 9,10-diol and 7,8-diol, but most of these diols were in the free form in the medium. The medium from cells treated with 3.75 nmol/ml BP has a quantitatively different profile, and most of the radioactivity obtained by extraction with organic solvent and digestion with beta-glucuronidase was eluted in the regions of phenols. These results show that in hamster embryo cells BP is mainly metabolised to conjugates of phenols with glucuronic acid.
研究了培养的仓鼠胚胎细胞对氚标记的苯并[a]芘（BP）水溶性代谢物的形成。水相中放射性与有机相中放射性的比值随孵育时间增加。在培养基中加入3.75 nmol/ml的[³H]BP孵育48小时后，超过90%的³H放射性出现在水相中，而BP浓度增加10倍时，约一半的放射性仍留在有机相中。通过高压液相色谱（HPLC）用乙酸乙酯从37.5 nmol/ml BP的培养基中提取的主要代谢物是9,10-二醇和7,8-二醇；但用β-葡萄糖醛酸酶处理培养基后，主要的氧化代谢物是酚类，9-羟基BP的量多于3-羟基BP。β-葡萄糖醛酸酶也释放出9,10-二醇和7,8-二醇，但这些二醇在培养基中大多以游离形式存在。用3.75 nmol/ml BP处理的细胞培养基具有不同的定量特征，通过有机溶剂萃取和β-葡萄糖醛酸酶消化获得的大部分放射性在酚类区域洗脱。这些结果表明，在仓鼠胚胎细胞中，BP主要代谢为酚类与葡萄糖醛酸的结合物。
