Ma P C, Lu X Y, Yang J J, Zheng Q T
Institute of Dermatology, Chinese Academy of Medical Sciences, Nanjing.
Yao Xue Xue Bao. 1991;26(10):759-63.
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.
从雷公藤（Tripterygium wilfordii Hook.f.）的根和叶中分离出一种新的二萜三环氧物，16-羟基雷公藤内酯醇。16-羟基雷公藤内酯醇为白色簇晶，熔点232 - 233.5℃。其分子式为C20H24O7。基于光谱数据（红外光谱、质谱、紫外光谱、1H-核磁共振、13C-核磁共振、二维核磁共振、核Overhauser效应）和X射线晶体学分析，确定16-羟基雷公藤内酯醇的结构和立体化学为L2。在药理筛选中，16-羟基雷公藤内酯醇表现出明确的抗炎作用以及较强的免疫抑制和抗生育活性。在抗炎作用方面，以巴豆油诱导小鼠耳肿胀模型，其半数有效剂量（ED50）为0.12mg/kg。在免疫抑制作用方面，以小鼠溶血素抗体形成模型，其ED50为0.05mg/kg。在抗生育作用方面，其最低有效剂量（口服）为0.027mg/kg×33天。
