Studies On The Chemical Constituents And Biological Activities Of The Seeds Of Euphorbia Lathyris

This thesis is composed of four chapters.The first chapter reviewed the resource distribution,traditional efficacy,chemical constituents and bioactivities of the genus Euphorbiae.In the second chapter,we summarized the study on the plant resource,chemical constituents,structure characteristic of ingenane and lathyrane diterpenoids and bioactivities of Euphorbia lathyris.The investigation on chemical constituents and bioactivities of seeds of E.lathyris collected from Hebei Province,was reported in chaper 3.The last chapter introduces the summary and expectation of my dissertation,and put forward my own points of view and gives suggestion for future research works.The seeds of Euphorbia lathyris,a common traditional Chinese medicine,have been used to treat hydropsy,ascites,terminal schistosomiasis and snakebites.It is widespread in Middle and Southern Europe and in Southern Russia and was introduced into Northern and Southern America and Australia.Previous chemical studies on this species yielded various diterpenoids,including ingenane and lathyrane types,but few of them showed detailed biological activities.Recent studies have shown that ingenol derivatives from the genus Euphorbia were demonstrated to be potent PKC activators as well as anticancer and anti-HIV agents,while Lathyrane derivatives are also well-known as apoptosis inducers and multidrug resistance modulators in cancer cells.To identify potential anti-HIV components in E.lathyris,we used HIV-1NL4-3 Luc as Drug screening cell model to screen for inhibitors of HIV virus replication.The 95%ethanol extract of the seeds of E.lathyris was suspended in water and partitioned with petroleum ether,ethyl-acetate and n-butyl alcohol.Bioassay showed that the active fraction existed in petroleum ether phase(EC501.2 ?g/ml),ethyl-acetate phase(EC501.1?g/ml)and n-butyl alcohol phase(EC50 0.18 ?g/ml).Combined with previous research experience,petroleum ether phase of this plant have been selected and investigated by means of bioassay-guided purification,which resulted in the isolation of diterpene esters of ingenane and lathyrane types.,four compounds showed obvious anti-tumor drug resistance reverse transcription activity.