Lissner R, Merk H, Bolsen K, Goerz G
Arzneimittelforschung. 1985;35(12):1825-7.
Theophylline induces increase of hepatic cytochrome P-450 contents and P-450 dependent polysubstrate monooxygenases (e.g. p-nitroanisol-demethylase, 7-ethoxycoumarin-deethylase) in rats and other animals and in man. The purpose of this study is to investigate the long-term effect of theophylline on hepatic cytochrome P-450 and P-450 dependent enzyme activities in rats. P-450 content is enhanced after 6 days treatment with theophylline (150 mg/kg/d orally), but reaches the initial level after 28 days treatment. However, the P-450 dependent enzyme activities (7-ethoxycoumarin-deethylase, p-nitroanisol-demethylase) remain elevated. The in vitro inhibition of 7-ethoxycoumarin-deethylase by alpha-naphthoflavone and metyrapone suggests a mixed type induction by theophylline. Treatment of the animals with phenobarbital and theophylline or with benzo(alpha)pyrene and theophylline does not lead to an enhancement of P-450 content compared with a treatment solely by phenobarbital or benzo(alpha)pyrene. However, the simultaneous application of theophylline and phenobarbital increases the 7-ethoxycoumarin-deethylase and p-nitroanisol-demethylase activities compared with an exclusive phenobarbital treatment, whereas the benzo(alpha)pyrene effect is not enhanced by theophylline.
茶碱可诱导大鼠、其他动物及人体肝脏细胞色素P-450含量及P-450依赖性多底物单加氧酶(如对硝基苯甲醚脱甲基酶、7-乙氧基香豆素脱乙基酶)增加。本研究的目的是探讨茶碱对大鼠肝脏细胞色素P-450及P-450依赖性酶活性的长期影响。用茶碱(150mg/kg/d口服)治疗6天后,P-450含量升高,但治疗28天后恢复至初始水平。然而,P-450依赖性酶活性(7-乙氧基香豆素脱乙基酶、对硝基苯甲醚脱甲基酶)仍保持升高。α-萘黄酮和甲吡酮对7-乙氧基香豆素脱乙基酶的体外抑制表明茶碱为混合型诱导剂。与仅用苯巴比妥或苯并(α)芘治疗相比,用苯巴比妥和茶碱或苯并(α)芘和茶碱治疗动物不会导致P-450含量增加。然而,与单独用苯巴比妥治疗相比,同时应用茶碱和苯巴比妥可增加7-乙氧基香豆素脱乙基酶和对硝基苯甲醚脱甲基酶的活性,而苯并(α)芘的作用不会因茶碱而增强。