雷公藤中16-羟基雷公藤内酯醇的分离与鉴定

从雷公藤(Tripterygium wilfordii Hook.f.)叶及根中分离出16-羟基雷公藤内酯醇(16-hydroxytriptolide,L₂).根据光谱(UV,IR,¹H-NMR,¹³C-NMR,2d-NMR及MS等)数据分析,推定其化学结构为L₂,并通过X-射线晶体分析确定了其结构和构型。该物是一个新化合物,具有较强的抗炎、免疫抑制和雄性抗生育作用。

16-Hydroxytriptolide, a new active diterpene isolated from Tripterygium wilford II]

A new diterpene triepoxide, 16-hydroxytriptolide was isolated from the root and leaves of Tripterygium wilfordii Hook.f. 16-Hydroxytriptolide was obtained as white cluster crystal, mp 232-233.5 degrees C. Its molecular formula is C20H24O7. The structure and stereochemistry of 16-hydroxytriptolide was established as L2 on the basis of spectral data (IR, MS, UV, 1H-NMR, 13C-NMR, 2d-NMR, NOE) and X-ray crystallographic analysis. In the pharmacologic screening, 16-hydroxytriptolide showed definite antiinflammatory actions and strong immunosuppressive and antifertile activities. In antiinflammatory action, its half effective dose (ED50) was 0.12 mg/kg with the model of croton oil induced ear swelling of mice. In immunosuppressive action, its ED50 was 0.05 mg/kg with the model of the formation of haemolysinantibody of mice. Its lowest effective dose (po) was 0.027mg/kg x 33d in antifertile action.