White J O, Moore P A, Marr W, Elder M G, Lim L
Biochem J. 1982 Oct 15;208(1):199-204. doi: 10.1042/bj2080199.
Progesterone therapy results in partial reversibility of histological abnormalities of the rat uterus exposed to constant oestrogen stimulation and is associated with a decrease in nuclear oestrogen receptor content, which may underlie the tissue response to hormone treatment [White, Moore, Elder & Lim (1982) Biochem. J. 202, 535-41]. The synthetic progestins norgestrel and norethisterone used in this study were as effective as progesterone in decreasing the content of nuclear oestrogen receptor. However, only norgestrel had an ameliorative effect on epithelial hyperplasia and metaplasia. The non-steroidal anti-oestrogen tamoxifen caused a significant decrease in both nuclear and cytosol oestrogen receptor content without any change in luminal epithelial hyperplasia and metaplasia. Each progestin caused an increase, whereas tamoxifen caused a decrease, in the proportion of nuclear oestrogen receptors that were unoccupied. Each compound caused a decrease in the content of cytosol progesterone receptor. The effectiveness of compounds used as oestrogen antagonists is discussed with reference to their mode of action.
孕酮治疗可使持续接受雌激素刺激的大鼠子宫组织学异常部分逆转，并与核雌激素受体含量降低有关，这可能是组织对激素治疗产生反应的基础[怀特、摩尔、埃尔德和林（1982年）《生物化学杂志》202卷，535 - 41页]。本研究中使用的合成孕激素炔诺孕酮和炔诺酮在降低核雌激素受体含量方面与孕酮效果相同。然而，只有炔诺孕酮对上皮增生和化生有改善作用。非甾体类抗雌激素他莫昔芬可使核雌激素受体和胞质雌激素受体含量显著降低，而管腔上皮增生和化生无任何变化。每种孕激素都会使未被占据的核雌激素受体比例增加，而他莫昔芬则使其降低。每种化合物都会使胞质孕酮受体含量降低。根据其作用方式对用作雌激素拮抗剂的化合物的有效性进行了讨论。
