Gupta S, Dhar J D, Dwivedi A, Bansode F W, Chowdhury S R, Setty B S
Division of Endocrinology, Central Drug Research Institute, Lucknow, India.
Endocr Res. 1998 May;24(2):171-84. doi: 10.1080/07435809809135526.
Studies with 85/287, a potent nonsteroidal antiestrogen/antiimplantation agent were taken up. In this paper we report alterations in uterine morphometric measurements and estrogen/progesterone receptor levels under the influence of this compound. Results showed 32% decline in stromal absolute volume density on day 5 post-coitum (p.c.) only, whereas eosinophilic leucocyte number decreased both on days 3 and 5 p.c. (41%) in treated rat uterus. Epithelial mitotic activity showed complete cessation both in control and treated rats on day 5 p.c. Under the influence of the compound both cytosolic and nuclear estrogen receptor (ERc and ERn) levels decreased on day 3 p.c., but on day 5 p.c. ERn increased significantly. A significant increase was however noticed in progesterone nuclear receptors (PRn) on day 5 p.c. On the whole our studies showed overall significant changes in uterine morphometric measurement/estrogen and progesterone receptor levels during the preimplantation period in rat under the influence of compound 85/287, causing asynchrony of events and thus failure of implantation.
开展了对强效非甾体抗雌激素/抗着床剂85/287的研究。在本文中,我们报告了在该化合物影响下子宫形态测量值及雌激素/孕激素受体水平的变化。结果显示,仅在交配后(p.c.)第5天,基质绝对体积密度下降了32%,而在处理过的大鼠子宫中,嗜酸性白细胞数量在交配后第3天和第5天均减少(41%)。在交配后第5天,对照大鼠和处理过的大鼠的上皮有丝分裂活性均完全停止。在该化合物的影响下,胞质和核雌激素受体(ERc和ERn)水平在交配后第3天下降,但在交配后第5天,ERn显著增加。然而,在交配后第5天,孕激素核受体(PRn)显著增加。总体而言,我们的研究表明,在化合物85/287的影响下,大鼠着床前期子宫形态测量值/雌激素和孕激素受体水平发生了总体显著变化,导致事件不同步,从而着床失败。