Rose G L, Dowsett M, Mudge J E, White J O, Jeffcoate S L
Department of Gynecology, Chelsea Hospital for Women, London, United Kingdom.
Fertil Steril. 1988 Feb;49(2):224-8. doi: 10.1016/s0015-0282(16)59706-4.
Danazol and gestrinone are effective drugs in the treatment of endometriosis. Their mechanism of action remains uncertain, but may be related to their androgenic activity. The authors examined the effect of danazol on human endometrial cells cultured in vitro, its two major metabolites, ethisterone and 2 hydroxymethyl ethisterone, gestrinone, and testosterone (T) at 1X and 10X expected plasma concentrations. Danazol and T suppressed growth by 20.8 and 25.0% (P less than 0.01), respectively, at the lower dose, and by 26.9 and 35.5% (P less than 0.01), respectively, at the 10-fold higher dose. No significant suppression of growth occurred with gestrinone, ethisterone, or 2 hydroxymethyl ethisterone. The results provide further evidence that danazol and T (but not gestrinone) may act by a direct effect on endometrial tissue.
达那唑和孕三烯酮是治疗子宫内膜异位症的有效药物。它们的作用机制尚不确定，但可能与其雄激素活性有关。作者研究了达那唑在预期血浆浓度的1倍和10倍时，对体外培养的人子宫内膜细胞、其两种主要代谢物炔诺酮和2-羟甲基炔诺酮、孕三烯酮及睾酮（T）的影响。较低剂量时，达那唑和T分别使生长抑制20.8%和25.0%（P<0.01），剂量高10倍时，分别使生长抑制26.9%和35.5%（P<0.01）。孕三烯酮、炔诺酮或2-羟甲基炔诺酮对生长无明显抑制作用。结果进一步证明，达那唑和T（而非孕三烯酮）可能通过对子宫内膜组织的直接作用发挥功效。
