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本文用小鼠模型,以等毒剂量,检测了从雷公藤中分离的7个环氧二萜内酯化合物的雄性抗生育活性及在有效阈剂量下对溶血素抗体生成的影响。结果表明:在7个化合物中,6个(T4、T7、8T、T9、T10、及L2)具有明确的抗生育活性,其中T7、T8、T10、L2有效阈剂量为1/40 LD50,T4、T9为1/60 LD50;而T11无此活性。实验再次证实化合物的抗生育活性与免疫抑制活性不可分割,但是所有活性化合物在阈值抗生育总剂量下均不抑制小鼠溶血素抗体生成。化合物单剂量的抗生育效价比抗炎效价高5~28倍,比免疫抑制效价高3~12倍,免疫抑制作用总剂量为阈值抗生育总剂量的0.9~1.8倍。最后对雷公藤抗生育活性的利用价值、对抗炎免疫治疗的影响及对小鼠模型作了讨论。
In this study, the male antifertility activity of seven epoxy diterpene lactones isolated from Tripterygium wilfordii was tested in a mouse model at equal dose levels and the effect on hemolysin antibody production at an effective threshold dose. The results showed that among the 7 compounds, 6 (T4, T7, 8T, T9, T10, and L2) had definite antifertility activity. The effective threshold doses of T7, T8, T10 and L2 were 1/40 LD50 and T4 , T9 1/60 LD50; T11 without this activity. Experiments again demonstrated that the compound’s anti-fertility and immunosuppressive activities are indivisible, but all the active compounds do not inhibit the production of mouse hemolysin antibodies at the total threshold dose of anti-fertility. The compound single-dose anti-fertility titer is 5-28 times higher than the anti-inflammatory potency, 3-12 times higher than the immunosuppressive potency, and the total dose of immunosuppression is 0.9-1.8 times of the total anti-fertility dose. Finally, the utility value of anti-fertility activity of Tripterygium wilfordii, the influence on anti-inflammatory immunotherapy and the mouse model were discussed.