雷公藤中16-羟基雷公藤内酯醇的分离与鉴定  

16-HYDROXYTRIPTOLIDE,A NEW ACTIVE DITERPENE ISOLATED FROM TRIPTERYGIUM WILFORD Ⅱ

作　　者：马鹏程[1] 吕燮余 杨晶晶[2] 郑启泰[2] 

机构地区：[1]中国医学科学院皮肤病研究所,南京210042 [2]中国医学科学院药物研究所,北京100050

出　　处：《药学学报》1991年第10期759-763,共5页Acta Pharmaceutica Sinica

基　　金：国家七.五攻关;国家自然科学基金

摘　　要：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,L_2).根据光谱(UV,IR,~1H-NMR,^(13)C-NMR,2d-NMR及MS等)数据分析,推定其化学结构为L_2,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。A new diterpene triepoxide, 16-hydroxytriptolide was isolated from the root and loves of Tripterygium wilfordii Hook.f. 16-Hydroxytriptolide was obtained as white cluster crystal, mp 232～233.5℃. Its molecular formula is C_(20)H_(24)O_7. The structure and stereochemistry of 16-hydroxytriptolide was established as L_2 (Fig. 1 )on the basis of spectral data (IR, MS, UV, ~1H-NMR, ^(13)C-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 (ED_(50)) was 0.12mg/kg with the model of croton oil induced ear swelling of mice. In immunosuppressive action, its ED_(50) was 0.05mg/kg with the model of the formation of haemolysinantibody of mice. Its lowest effective dose (po) was 0.027mg/kg×33d in antifertile action.

关 键 词：雷公藤 二萜内酯 抗生育作用 

分 类 号：R282.710.5[医药卫生—中药学]