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Objective To observe the therapeutic effect and side reactions of Tripterygium wilfordii Hook.f. (GTW) glycosides on patients with uterine leiomyomas. Methods 65 normally cycling women with symptomatic uterine leiomyomas received 40mg daily dose GTW for 3 to 6 months. Baseline ultrasound tests were obtained to evaluate the sizes of myomas and uterus, then repeated three and six months after treatment. Blood samples were collected to determine the hormonal levels of in the mid-follicular and mid-luteal phases of the menstrual cycles before GTW therapy and at 3 ～ 4 months and 5 ～ 6 months after treatment. Results Significant decrease in leiomyoma volume was shown in 39 of 65 (60%) and 28 of 40 ( 70% ) patients after 3 ～ 4 months and 5 ～ 6 months of treatment, respectively. The decrease of the volume of leiomyoma was time-dependent as while 27. 84% and 51.60% in 3 ～ 4 months and 5 ～ 6months, respectively. 25 of 65 patients had amenorrhea during the course of treatment. Tripterygium wilfordii glycosides treatment induced a significant increase in LH and FSH levels (P ＜0.01 ) as compared with pretreatment values. In contrary, a significant decrease in E2 and P levels ( P ＜0. 05) was found, but no changes were observed in T and PRL levels after treatment. Conclusion Tripterygium wilfordii might serve as an effective therapeutic agent for leiomyomas with fewer side effects. A reversible inhibitory effect on the ovary by Tripterygium wilfordii glycosides may be one of the mechanisms of Tripterygium wilfordii in decreasing leiomyoma volume.