摘要
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。
The half-effective dose(ED50)、 therapeutic index(TI) and certain safety factor(CSF) of 7 diterpene lactone epoxide compounds with antiinflammatory and immunosuppressive action extracted from Tripterygium wilfordii (TW) were assayed using croton oil-induced ear swelling and hemolysin-antibody formation mouse models.The results indicated that triptolide(T10). trpchlorolide(T4)、triptonide(T7)、 tripdiolide(T8), triptolidenol(T9) and 16-hydroxytriptolide(L2) possessed both anti-inflammatory and immunosuppressive activities, while triptriolide(T11) had antiinflammatory activity only. The TI of the antiinflammatory action of 7 compounds were arranged in following order:T11(> 19), T10(17)、 T9(9.6)、T4(9.0)、 T8(7.3)、 L2(6.6)、 T7(5.9)、 while the TI of the immunosuppressive action of 6 compounds were arranged in following order: T9(30.7)、 T4(16.7)、 L2(15.8)、 T10(l3.7)、 T8(8.8)、 T7(7.5). The CSF parameters of both the activities of 7 compounds were all higher than 1. In which, the CSF of the immunosuppressive action of T9?T4 and L2 were 7.1、5.1 and 3.6 respectively. These facts clearly demonstrate that the antiinflammatory and immunosuppressive compounds in TW are pluralistic. These differences among these compounds can be used as one of the bases for the evaluation and selection of these compounds.The above experiments conclude that the practical value of these compounds, however, will also depend on their content and yield rate in the herb, on the degree of difficulty in synthesizing these compounds, and on difficulty involved in the preparation of their derivatives. The future of these compounds will depend on the results of genetic toxicology studies as well.
出处
《中国医学科学院学报》
CAS
CSCD
北大核心
1991年第6期398-403,共6页
Acta Academiae Medicinae Sinicae
基金
国家自然科学基金
关键词
雷公藤
环氧二萜内酯
抗炎
抗生育
Tripterygium wilfordii. diterpene lactone expoxide antiinflammatory immunosuppressive therapeutic index cartain safety factor
