Investigation Of The Chemical Constituents And Biological Activities Of Thermopsis Lupinoides And The Daphne Tangutica

Thermopsi.s lupinoides belongs to the genus Thermopsis of the Leguminosae family,which is mainly distributed in Amur,Jilin and the northwestern region of China.It has the effect of expectorant and antitussive,and has been traditionally used for the treatment of various diseases,such as poisoning,edema,vomiting,and various sores and sores.More importantly,its extract has anti-cancer,anti-bacterial,immunological,anti-oxidative and anti-influenza pharmacological activities.Daphne tangutica Maxim is a traditional Chinese medicine belongs to the family Thymelaeaceae distributed mainly in Shanxi and Gansu provinces.Its extract has the effects of nourishing kidney deficiency,replenishing yang,diuresis,protecting liver and improving eyesight.And it has long been used as the folk medicine to treat enuresis,urinary dysfunction,dizziness,and lack of yang,Based on reviewing of the previous research results about the chemical constitutents and biological activities of genuses Tkhermopsis and Stellera,we have investigated the chemical constitLuents of Thermopsis lupinoides and Daphne tangutica collected from county of Tongwei,Gansu province.In addition,the anticancer and antioxidation activities of the partical isolated compounds were also evalutated.And the major results are summarized as following:(1)6 known alkaloids(1-6)were isolated from the ethanol extract of the whole plant of Thermopsis lupinoides by using various spectroscopic techniques,such as regular pressure silica gel column,TLC,Sephadex LH-20 gel column and HPLC.Their chemical stuctues were elucidated as Thermospine(1),N-methylcytisine(2),Cytosine(3),Anagyrine(4),N-formylcytisine(5),Protoberine(6)by detailed analysis of the spectroscopy data,including 1H,13C NMR,1H-1H COSY,HSQC,HMBC,FT-IR and Ms,together with in comparison with the literatures.Among them,compounds 1 and 4 enantiomers isolated from Thermopsis lupinoides and compounds 5 and 6 were isolated from this plant for the first time.In addition,two compounds(7)and(8)were purified from the roots of Daphne tangutica.(2)Their antioxidant activities were evaluated by Ferric reducing antioxidant power(FRAP)assay for compounds 1,4,and 7 at 700 nm,using ascorbic acid(Vc)as a positive control.The results indicated that compounds 1,4,and 7 have dose-response antioxidant activity.(3)Compound 1,4,7 were also selected to evaluate the anticancer activity against human ovarian cancer cell line A2780 by MTT assay.The results indicated that compound 1 has no inhibitory effect on A2780 cells line.While its enantiomers compound 4 exhibited morderate anti cancer activity with IC5o of 57.14 ?M for A2780 cancer cells,suggesting that the 11-R configuration of quinolizidine alkaloids possess more potential anticancer application.Compound 7 displayed a moderate inhibitory effect on A2780 cells line with with IC50 of 25.6?M.