In vivo characterization of progestins with reduced non-genomic activity in vitro.

C Otto, B Rohde-Schulz, G Schwarz, I Fuchs, M Klewer, H Altmann, K H Fritzemeier
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Abstract

Postmenopausal women that still have an uterus and suffer from hot flushes are treated with combinations of estrogens and progestins. Whereas estrogens are indispensable for treating postmenopausal symptoms, progestins are added to counteract the proliferative activity of estrogens on uterine epithelial cells. However, in the mammary gland, progestins, given together with estrogens, stimulate the proliferation of mammary epithelial cells. Therefore, progestins with reduced proliferative activity in the mammary gland would be of advantage for hormone therapy of postmenopausal women. In order to identify progestins with better tissue-selectivity, we exploited the activation of different signal transduction pathways by the classical progesterone receptor. We demonstrated that progestins with reduced non-genomic versus genomic activity in vitro show a better dissociation of uterine versus mammary gland effects in vivo than medroxyprogesterone acetate (MPA), a synthetic progestin that is widely used in hormone therapy.

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体外非基因组活性降低的孕激素的体内表征。
绝经后仍有子宫并患有潮热的妇女可以用雌激素和黄体酮联合治疗。虽然雌激素对于治疗绝经后症状是必不可少的,但添加孕激素是为了抵消雌激素对子宫上皮细胞的增殖活性。然而,在乳腺中,黄体酮与雌激素一起使用会刺激乳腺上皮细胞的增殖。因此,降低乳腺增殖活性的黄体酮将有利于绝经后妇女的激素治疗。为了鉴定具有更好组织选择性的黄体酮,我们利用了经典黄体酮受体激活的不同信号转导途径。我们证明体外非基因组活性和基因组活性降低的孕激素在体内比醋酸甲羟孕酮(MPA)表现出更好的子宫和乳腺分离作用,醋酸甲羟孕酮是一种广泛用于激素治疗的合成孕激素。
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