Hietanen E, Laitinen M, Koivusaari U
Enzyme. 1980;25(3):153-7. doi: 10.1159/000459241.
The inducibility of the mucosal drug-metabolizing enzymes of rat small intestine was studied by administering 3-methylcholanthrene either intragastrically or intraperitoneally. The aryl hydrocarbon hydroxylase activity was 4.1 times higher after intragastric than after intraperitoneal administration of methylcholanthrene. The ethoxycoumarin-O-diethylase activity was 11 times and UDP-glucuronosyltransferase (with p-nitrophenol as substrate) activity was 3 times higher after intragastric administration than after intraperitoneal administration. The epoxide hydratase activity was, on the other hand, 38% lower after intragastric administration of 3-methylcholanthrene than after intraperitoneal administration. The results suggest that compounds entering the body intragastrically, e.e. in the diet, might have profound enzyme-specific effects on the intestinal metabolic rates of drugs.
通过胃内或腹腔内给予3-甲基胆蒽，研究大鼠小肠黏膜药物代谢酶的诱导性。给予甲基胆蒽后，胃内给药组的芳烃羟化酶活性比腹腔内给药组高4.1倍。胃内给药组的乙氧香豆素-O-二乙酶活性比腹腔内给药组高11倍，以对硝基苯酚为底物的UDP-葡萄糖醛酸转移酶活性比腹腔内给药组高3倍。另一方面，胃内给予3-甲基胆蒽后，环氧化物水化酶活性比腹腔内给药组低38%。结果表明，经胃内进入体内的化合物，如饮食中的化合物，可能对药物的肠道代谢率产生深刻的酶特异性影响。
