[Structure modification of triptolide, a diterpenoid from Tripterygium wilfordii].
In this paper, the structure modification of triptolide was studied and nine triptolide 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 triptolide with HCl in acetone under mild condition.
Yu
D Q
DQ
Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing.
Zhang
D M
DM
Wang
H B
HB
Liang
X T
XT
D000818:Animals; D000917:Antibody Formation / Q000187:drug effects; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004365:Drugs, Chinese Herbal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008213:Lymphocyte Activation / Q000187:drug effects; D051379:Mice; D010616:Phenanthrenes; D013329:Structure-Activity Relationship
D004224:Diterpenes; D004365:Drugs, Chinese Herbal; D010616:Phenanthrenes; C068051:tripchlorolide; C080716:tripbromolide