Aitio A, Ahotupa M, Parkki M G
Eur J Drug Metab Pharmacokinet. 1980;5(1):35-40. doi: 10.1007/BF03189441.
The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubin was found to be activated by manganese, cobalt, nickel, cadmium, mercury and lead ions in native microsomes, but not in digitonin-treated microsomes. Aluminum, ferrous iron, cadmium, barium and lead increased the conjugation of 4-nitrophenol in native microsomes and aluminium in digitonin-treated microsomes as well. Lead slightly activated 4-methylumbelliferone conjugation, whereas none of the metal salts studied were found to activate the conjugation of 2-aminophenol. Copper and zinc salts inhibited all conjugations. In digitonin-treated microsomes, the conjugation of 4-nitrophenol was inhibited by cadmium and mercury, that of 4-methylumbelliferone by nickel and lead as well. The sensitivity of 4-methylumbelliferone conjugation to inhibition by mercury was most pronounced in microsomes prepared from rats pretreated with 2,3,7,8-tetrachlorodibenzo-p-dioxin.
体外研究了铝、锰、亚铁离子、铁离子、钴、镍、铜、锌、镉、钡、汞和铅离子对大鼠肝脏尿苷二磷酸葡萄糖醛酸基转移酶活性的影响，该酶作用于4-甲基伞形酮、4-硝基苯酚、胆红素和2-氨基苯酚。发现胆红素的结合在天然微粒体中被锰、钴、镍、镉、汞和铅离子激活，但在洋地黄皂苷处理的微粒体中未被激活。铝、亚铁离子、镉、钡和铅增加了天然微粒体中4-硝基苯酚的结合，以及洋地黄皂苷处理的微粒体中铝的结合。铅略微激活了4-甲基伞形酮的结合，而所研究的金属盐均未激活2-氨基苯酚的结合。铜盐和锌盐抑制了所有的结合反应。在洋地黄皂苷处理的微粒体中，镉和汞抑制了4-硝基苯酚的结合，镍和铅也抑制了4-甲基伞形酮的结合。在用2,3,7,8-四氯二苯并对二恶英预处理的大鼠制备的微粒体中，4-甲基伞形酮结合对汞抑制的敏感性最为明显。
