二苯硫代乙内酰脲致甲状腺肿作用机制的研究。

Studies on the mechanism of goitrogenic action of diphenylthiohydantoin.

作者信息

Tsukui T, Aizawa T, Yamada T, Kawabe T

出版信息

Endocrinology. 1978 Jun;102(6):1662-9. doi: 10.1210/endo-102-6-1662.

Abstract

Diphenylthiohydantoin (DPTH) is a potent goitrogenic compound and produces goiters in rats. Like methimazole, DPTH depresses plasma T4 and T3 concentrations and elevates plasma T4 and T3 concentrations and elevates plasma TSH concentration. Unlike methimazole, however, DPTH does not suppress thyroidal radioiodine uptake and thyroid hormone synthesis, although the monoiodotyrosine to diiodotyrosine ration is elevated by DPTH. DPTH does not inhibit thyroidal radioiodine release or augment the degradation of thyroid hormone. DPTH depresses an increase of plasma T4 and T3 in thyroidectomized rats maintained on T4 or T3 by augmenting fecal excretion of hormones. In addition, DPTH decreases conversion of T4 to T3 in vitro. It is suggested that DPTH is a unique goitrogen which acts at two different extrahyroidal sites, viz. fecal loss of thyroid hormone and conversion of T4 to T3.

摘要

二苯硫代乙内酰脲（DPTH）是一种强效致甲状腺肿化合物，可在大鼠体内引发甲状腺肿。与甲巯咪唑一样，DPTH会降低血浆T4和T3浓度，并升高血浆促甲状腺激素（TSH）浓度。然而，与甲巯咪唑不同的是，尽管DPTH会提高单碘酪氨酸与二碘酪氨酸的比例，但它不会抑制甲状腺对放射性碘的摄取和甲状腺激素的合成。DPTH不会抑制甲状腺放射性碘的释放，也不会增强甲状腺激素的降解。通过增加激素的粪便排泄，DPTH会降低甲状腺切除术后用T4或T3维持的大鼠血浆T4和T3的升高。此外，DPTH在体外会降低T4向T3的转化。有人认为，DPTH是一种独特的致甲状腺肿物质，作用于两个不同的甲状腺外部位，即甲状腺激素的粪便流失以及T4向T3的转化。