Studies On Chemical Constituents And Multidrug Resistance Reversal Of Tripterygium Hypolaucum

Tumor is the leading killer of human health and life.Drug chemotherapy,as the main means of treating tumors,has a good effect.However,in the process of drug chemotherapy,tumor cells tend to gradually develop "adaptability" to drugs,and multidrug resistance(mutidrug resistance,MDR)appears.Therefore,it is necessary to seek treatment methods and drugs with good curative effect and low toxicity from natural products.Traditional Chinese medicine has become a hotspot in the research of anti-tumor drugs due to its advantages of abundant drug sources,low price and long application history.Tripterygium hypolaucum of the genus Tripterygium(Celastraceae),is a traditional Chinese medicine(TCM)for the treatment of rheumatoid arthritis and lupus erythematosus disease,which mainly includs sesquiterpenes,diterpines,triterpenes,and lignans.Pharmacological research shows that T.hypolaucum has anti-tumor,immunosuppressants,anti-inflammatory and other effects.In previous studies,we found that dihydroagarofuran sesquiterpenes has significant anti-tumor and anti-multidrug resistance activities,which aroused our interest.In this paper,the chemical constituents of the stems and leaves of T.hypolaucum from the Cangshan of Dali,Yunnan province,and the biological activities of reversal of multidrug resistance of tumors were systematically studied,and 41 compounds were isolated and identified by a variety of chromatographic separation techniques and modern spectroscopy methods including 12 new dihydroagarofuran sesquiterpenoids and a new abietane diterpene.At the same time,we screened the isolated compounds reversed the HepG2/ADR tumor multidrug resistance activity.Compounds 10,15 and 20 showed weaker reversal of HepG2/ADR tumor resistance activity in combined with ADR at the concentration of 20 ?M(RF = 7.4~14.6).Compounds 13 and 14 showed moderate reversal of HepG2/ADR tumor resistance activity(RF = 73.5 and 59.8,respectively)when combined with ADR at a concentration of 20 ?M,and while compounds 1 and 2 showed significant reversal ofHepG2/Adr tumor resistance activity when combined with ADR at 20 ?M concentration(reversal factor RF = 102 and 200,respectively).