Danazol inhibits aromatase activity of endometriosis-derived stromal cells by a competitive mechanism
Danazol inhibits aromatase activity of endometriosis-derived stromal cells by a competitive mechanism
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DOI：
10.1016/j.fertnstert.2005.12.074
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发表时间：
2006-08-01
影响因子：
6.7
通讯作者：
Inoue, Masaki
中科院分区：
文献类型：
--
作者：
Murakami, Koichi;Nomura, Kazuhito;Inoue, Masaki
目的：评价达那唑对子宫内膜异位症雌激素（E）产生的抑制作用。设计：前瞻性随机研究。设置：一所大学医院妇产科的学术研究单位。患者：13例子宫内膜异位症患者。干预：达那唑加入到子宫内膜异位症衍生的基质细胞或巧克力囊肿制备的微粒体悬浮液的培养物中。主要结果测量：结果：达那唑（Danazol）浓度大于10（-6）M时，在基础和前列腺素E-2（PGE（2））刺激条件下，可显著抑制子宫内膜异位症基质细胞芳香化酶活性。达那唑（10（-5）M）不影响芳香化酶的mRNA和蛋白水平。Danazol竞争性抑制子宫内膜异位症基质细胞芳香化酶活性（Ki值为1.7 × 10 ~（-6）M，Ki ′值为2.9 × 10 ~（-5）M）。结论：Danazol竞争性抑制子宫内膜异位症基质细胞芳香化酶活性，但不影响芳香化酶的mRNA或蛋白水平。这些结果表明达那唑局部应用于前列腺病变的疗效。
Objective: To evaluate the inhibitory effect of danazol on estrogen (E) production in endometriosis.Design: Prospective randomized study.Setting: Academic research unit of the department of obstetrics and gynecology in a university hospital.Patient(s): Thirteen patients with endometriosis.Intervention(s): Danazol was added to the culture of endometriosis-derived stromal cells or suspensions of microsomes prepared from chocolate cysts.Main Outcome Measure(s): The aromatase activities as well as mRNA and protein levels of aromatase in endometriosis-derived stromal cells or microsomes of endometriosis were examined.Result(s): Danazol treatment with a concentration greater than 10(-6) M significantly suppressed aromatase activity of endometriosis-derived stromal cells under basal and prostaglandin E-2 (PGE(2))-stimulated conditions. Danazol (10(-5) M) did not affect mRNA and protein levels of aromatase. Danazol competitively inhibited aromatase activity (by 1.7 X 10(-6) M of calculated Ki and 2.9 X 10(-5) M of Ki') of endometriosis microsomes.Conclusion(s): Danazol competitively inhibited aromatase activity in endometriosis-derived stromal cells without affecting either the mRNA or protein levels of aromatase. These results indicate the efficacy of local application of danazol to endometriotic lesions.