Hepatic UDP-glucuronyltransferase(s) activity toward thyroid hormones in rats: induction and effects on serum thyroid hormone levels following treatment with various enzyme inducers.
Hepatic UDP-glucuronyltransferase(s) activity toward thyroid hormones in rats: induction and effects on serum thyroid hormone levels following treatment with various enzyme inducers.
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大鼠肝脏 UDP-葡萄糖醛酸转移酶对甲状腺激素的活性：用各种酶诱导剂治疗后的诱导及其对血清甲状腺激素水平的影响。
DOI：
10.1016/0041-008x(91)90138-5
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发表时间：
1991
影响因子：
3.8
通讯作者：
H. Yamada
中科院分区：
文献类型：
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作者：
K. Saito;H. Kaneko;K. Sato;A. Yoshitake;H. Yamada
在雄性 Sprague-Dawley 大鼠中连续 4 次注射 75-150 mg/kg/天的各种肝酶诱导剂后，检查了对甲状腺激素的肝 UDP-葡萄糖醛酸转移酶 (hUDP-GT(s)) 活性的诱导以及活性与血清甲状腺激素或促甲状腺激素 (TSH) 水平之间的关系。 hUDP-GT 对甲状腺素 (T4; hUDP-GT-T4) 的活性是通过用 β-萘黄酮、3-甲基胆蒽 (3-MC)、多氯联苯或孕烯醇酮-16α-甲腈处理诱导的。然而，异黄樟素给药没有观察到显着的诱导，而在苯巴比妥和1,1,1-三氯-2,2-双(对氯苯基)乙烷的情况下，发现轻微的减少。这些诱导剂的 hUDP-GT-T4 诱导曲线与 hUDP-GT 对三碘甲状腺原氨酸（T3；hUDP-GT-T3）的活性大致相同，表明这两种甲状腺激素（T4 和 T3）被相同的 hUDP-GT 葡萄糖醛酸化。此外，hUDP-GT-T4和hUDP-GT-T3的诱导曲线与hUDP-GT对1-萘酚的诱导曲线相似，但与氯霉素不同，这表明T4和T3属于所谓的1组底物，其优先被3-MC处理诱导的hUDP-GT葡萄糖醛酸化。血清T4水平的降低与hUDP-GT-T4活性的增加明显相关，表明血清T4水平直接受到hUDP-GT-T4活性的影响。然而，未发现甲状腺激素水平下降与 TSH 水平代偿性上升之间存在直接相关性。
Induction of hepatic UDP-glucuronyltransferase(s) (hUDP-GT(s)) activity toward thyroid hormones and the relationship between the activity and the serum thyroid hormones or the thyroid stimulating hormone (TSH) level were examined in male Sprague-Dawley rats after four consecutive ip doses of various hepatic enzyme inducers at 75–150 mg/kg/day. hUDP-GT activity toward thyroxine (T4; hUDP-GT-T4) was induced by treatment with β-naphthoflavone, 3-methylcholanthrene (3-MC), polychlorinated biphenyls, or pregnenolone-16α-carbonitrile. However, no significant induction was observed for isosafrole administration and in the cases of phenobarbital and 1,1,1-trichloro-2,2-bis(p-chlorophenyl)ethane slight decreases were found. The induction profile of hUDP-GT-T4for these inducers was approximately the same as that of hUDP-GT activity toward triiodothyronine (T3; hUDP-GT-T3), indicating that these two thyroid hormones (T4and T3) are glucuronidated by the same hUDP-GT(s). Moreover, the induction profile of both hUDP-GT-T4and hUDP-GT-T3was similar to that of hUDP-GT toward 1-naphthol, but not chloramphenicol, suggesting that T4and T3belong to the so-called group-1 substrates which are preferentially glucuronidated by hUDP-GT(s) inducible by treatment with 3-MC. Decreases in serum T4levels clearly correlated with an increase in hUDP-GT-T4activity, inducating that serum T4levels are directly affected by hUDP-GT-T4activity. However, no direct correlation between decrease in thyroid hormone levels and compensatory increase in TSH levels was found.
大鼠肝脏UDP-葡萄糖醛酸基转移酶功能异质性的诱导研究。
影响因子：
3.8
作者：
Watkins,JB;Gregus,Z;Thompson,TN;Klaassen,CD
通讯作者：
Klaassen,CD
在输注甲状腺激素的甲状腺切除大鼠中，血清促甲状腺素浓度与血清三碘甲状腺原氨酸浓度的相关性高于与血清甲状腺素浓度的相关性。
影响因子：
4.8
作者：
Emerson,CH;Lew,R;Braverman,LE;DeVito,WJ
通讯作者：
DeVito,WJ
UDP-葡萄糖醛酸基转移酶对洋地黄毒甙元-单洋地黄苷的活性。
DOI：
--
发表时间：
1988
期刊：
Drug metabolism and disposition: the biological fate of chemicals
影响因子：
--
作者：
Hazelton,GA;Klaassen,CD
通讯作者：
Klaassen,CD