米非司酮治疗子宫肌瘤的临床疗效及机理探讨

Mechanism and effectiveness or mifepristone in treatment of uterine leiomyomata

探讨米非司酮（Ru486）治疗子宫肌瘤的临床疗效和机理。方法：应用国产的Ru48625mg／d，治疗39例子宫肌瘤Ⅰ～Ⅱ疗程，B超定期随访子宫肌瘤及子宫体积，放免法监测血性激素水平，Northernblot法和HAP单点饱和分析法检测瘤心、瘤边缘及正常子宫肌组织中的ERmRNA、PRmRNA表达和ER、PR蛋白含量。结果：Ⅰ疗程肌瘤体积明显缩小53．88％，Ⅱ疗程缩小达61．20％，临床总有效率为84．62％。服药前后血性激素水平处于早期滤泡期水平，Ru486治疗后肌瘤和正常子宫肌组织中的PRmRNA表达及PR蛋白含量均显著降低（P＜0.01）。结论：Ru486有可逆性抑制PR及其基因表达作用，同时抑制性腺轴，使肌瘤明显缩小。此疗法有效，副作用小，可重复使用。

Objective:To investigate the effectiveness of Ru486 in the treatment of leiomyomata and its mechanismof action. Methods: By observation of the effect of Ru486, a domestic product, at a daily dosage of 25mg for 3～6months in 39 women with leiomyomata. Ultrasonic measurements of leiomyomata and uterine volume were made beforeand after the treatment monthly. Serum levels of hormones were determined by radioimmunoassay. Expression ofERmRNA,PRmRNA and ER, PR proteins at the center of myomatous tissue, marginal area and myometrium were determined by Northern blot and HAP of single-dose analysis. Results: Significant decrease in leiomyomata volume wasshown (53. 88% ) after 3 months of Ru486 treatment and 61. 20% after 6 months of treatment. The total effective ratewas 84. 62%. Serum hormonal levels were similar to those in the early follicular phase before and after treatment. Theexpression of PRmRNA,PR protein levels in leiomyomata and myometrium were significantly decreased after administration of Ru486(P<0.01). Conclusions:The above study suggests Ru486 also inhibits the gonadal axis which leads tothe reduced size of myomata, is not only related to interference of cyclic ovulatory action but also suppression on PR andexpression of PRmRNA. The suppression is at the level of transcription level. This treatment has few side effects andcan be repeatedly used.