摘要
为降低雷公藤内酯醇的毒性,寻找高效低毒的抗炎免疫化合物,对雷公藤内酯醇(trip-tolide,1)的结构进行了修饰,合成了九个雷公藤内酯醇衍生物。初步活性测定显示雷公藤氯内酯(tri-pchlorolide,2)和雷公藤溴内酯醇(tripbromolide,3)的免疫抑制活性与雷公藤内酯醇近似,但毒性有所降低。其他化合物的活性大大低于雷公藤内酯醇。
In this paper, the structure modification of triptolide was studied and nine trip
tolide derivatives were synthesized. A preliminary test for the immunosuppression activity in vitro
showed that tripchlorolide (2) and tripbromolide (3) have strong activity similar to triptolide, while
their toxicity are much lower. The activity of other compounds was decreased significantly. A simple
method for the preparation of tripchlorolide from triptolide in 92% yield was found by reacting trip
tolide with HCl in acetone under mild condition.
出处
《药学学报》
CAS
CSCD
北大核心
1992年第11期830-836,共7页
Acta Pharmaceutica Sinica
关键词
雷公藤
内酯醇
免疫抑制活性
Triptolide
Tripchlorolide
Immunosuppression activity
