达那唑与孕酮受体结合，并在体外抑制人子宫内膜癌细胞的生长。
Danazol binds to progesterone receptors and inhibits the growth of human endometrial cancer cells in vitro.
作者信息
Ikegami H, Terakawa N, Shimizu I, Kano H, Tanaka Y, Aono T, Tanizawa O, Matsumoto K
出版信息
Am J Obstet Gynecol. 1986 Oct;155(4):857-61. doi: 10.1016/s0002-9378(86)80039-4.
Based on our recent findings that danazol, an isoxazol derivative of ethinyltestosterone, has a profound growth-inhibitory effect on an established human endometrial adenocarcinoma cell line, the effects of danazol on cancer cells from human endometrial adenocarcinomas obtained by hysterectomy were investigated in the present study. Of the 22 uterine adenocarcinomas, estrogen, progesterone, and androgen receptors were found in 12, 14, and 4 tumors, respectively. Competitive binding studies showed that danazol specifically binds to progesterone and androgen receptors but not to estrogen receptors. Of the five cancer cells from five patients succeeded in primary cell culture, a marked inhibition of cell growth was demonstrated by addition of danazol in two cancer cells having progesterone but not androgen receptors. However, danazol did not affect the growth of the remaining three cancer cells lacking progesterone receptors. These results strongly suggest that danazol has a significant growth-inhibitory effect on human endometrial adenocarcinoma cells, possibly through progesterone receptors in the cells.
基于我们最近的研究发现，炔诺酮（乙炔睾酮的异恶唑衍生物）对已建立的人子宫内膜腺癌细胞系具有显著的生长抑制作用，本研究调查了炔诺酮对通过子宫切除术获得的人子宫内膜腺癌癌细胞的影响。在22例子宫腺癌中，分别在12例、14例和4例肿瘤中发现了雌激素、孕激素和雄激素受体。竞争性结合研究表明，炔诺酮特异性结合孕激素和雄激素受体，而不结合雌激素受体。在成功进行原代细胞培养的5例患者的5个癌细胞中，在两个具有孕激素但不具有雄激素受体的癌细胞中加入炔诺酮后，显示出明显的细胞生长抑制。然而，炔诺酮对其余三个缺乏孕激素受体的癌细胞的生长没有影响。这些结果强烈表明，炔诺酮对人子宫内膜腺癌细胞具有显著的生长抑制作用，可能是通过细胞中的孕激素受体实现的。
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