Synthesis, Characterization Of Ursolic Acid And Oleanolic Acid Derivatives

Malignant neoplasm is general and frequently-occurring disease which threatens human health seriously. Many scientists over the world are very interested in that the natural products as lead compounds are modified to synthesis novel anti-tumor agents.Ursolic acid and oleanolic acid, as pentacyclic triterpenoids, are functional components of multiple natural product, and belongs to triterpenic acid, they consist in the nature as natural active products and exhibit various biological activities. Their structures are very similar and they are all potential anti-tumor promoters and cytotoxic agents against tumor cells, inhibiting proliferation, inducing apoptosis and preventing invasion. According to the existing research,ursolic acid and oleanolic acid also have anti-inflammation, anti-bacteria and hypolycemic pharmacological actions,their anti-tumor action have been established, so they can be researched to be a new anticarcinogen of availability. Because of the pharmacological activity, small side effect and hypotoxicity, they has been researched massively in the term of abstract,content determination and pharmacological actions, but there is few report about the structure activity relations of them and theirs derivatives.The natural product ursolic acid and oleanolic acid with anti-tumor activity,were taken as the lead compounds for modifying theirs structure in this dissertation. According to organic chemistry theory, advanced technique, new methods and results of bio-activity screenings, optimization of lead compounds' structure was carried out in order to develop new drug candidate or lead compounds with low toxicity, high activity, stabilization and controllable quality. By this research, 23 triterpenoid derivants have been prepared by structural modification of ursolic acid and oleanolic acid,and most of them are new compounds.