雷公藤抗炎免疫及抗生育活性分份的筛选：Ⅲ,7个环氧...

Screening of active anti-inflammatory, immunosuppressive and antifertility components of Tripterygium wilfordii. III. A comparison of the antiinflammatory and immunosuppressive activities of 7 diterpene lactone epoxide compounds in vivo]

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), tripchlorolide(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(greater than 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(13.7), 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.