Boutin J A, Batt A M, Siest G
Xenobiotica. 1983 Dec;13(12):755-61. doi: 10.3109/00498258309052237.
Six hydroxylated substrates were examined as potential inducers of UDP-glucuronosyltransferases towards their conjugation and the conjugation of other 'model' aglycones with glucuronic acid. Time-dependence (4, 14 and 28 days) and dose-dependence of treatments (from 25 mg/kg to 1 g/kg) were examined for some of these compounds. Monoterpenoid alcohols (borneol and terpineol) did not enhance the glucuronidation of the ten substrates tested. p-Hydroxybiphenyl gives typical 'substrate-induction' towards its own conjugation. Eugenol, a previously described inducer of UDP-glucuronosyltransferase activities in mouse, and 4-methylumbelliferone, give a general enhancement of all activities tested, especially those of the '3-methylcholanthrene-inducible' group of aglycones. p-Nitrophenol at low dose (2.5 mg/kg) gives a limited 'polycyclic aromatic hydrocarbon'-like increase.
研究了六种羟基化底物作为UDP-葡萄糖醛酸基转移酶对其结合以及其他“模型”苷元与葡萄糖醛酸结合的潜在诱导剂。对其中一些化合物研究了处理的时间依赖性(4、14和28天)和剂量依赖性(从25mg/kg至1g/kg)。单萜醇(冰片和萜品醇)未增强所测试的十种底物的葡萄糖醛酸化。对羟基联苯对其自身的结合表现出典型的“底物诱导”。丁香酚(一种先前描述的小鼠UDP-葡萄糖醛酸基转移酶活性诱导剂)和4-甲基伞形酮,对所有测试活性均有普遍增强作用,尤其是“3-甲基胆蒽诱导型”苷元组的活性。低剂量(2.5mg/kg)的对硝基苯酚产生有限的“多环芳烃”样增加。