Studies On The Chemical Constituents And Bioactivities Of Fissistigma Tungfangense

Fissistigma tungfangense belongs to Fissistigma of Annonaceae.Because of the rich in antitumor active ingredients,the plants of Fissistigma are widely concerned by scholars all around the world.Multiple types of compounds,including flavonoids,lignans,alkaloids,terpenoids and so on,were isolated from the roots,stems,leaves,and fruits of Fissistigma.Among these compounds,most of the alkaloids have good antitumor activity.Hitherto,studies on chemical composition and pharmacological activity of the domestic Fissistigma are relatively few,especially the lack of systemic study of alkaloids.And the pharmacological activities of Fissistigma have not been studied in depth.In order to exploit and utilize the Fissistigma further and clarify the pharmacophore basis of them,this study is on the alkaloids and antirheumatoid arthritis activity of the roots of Fissistigma tungfangense.A total of 92 compounds,including five skeleton types: alkaloids,flavonoids,sesquiterpenoids,phenylproanoids and other compound,were isolated from Fissistigma tungfangense through column chromatography over Silica gel,Sephadex LH-20,recrystallization and semi-preparative HPLC.On the basis of spectroscopic methods including NMR,MS,IR and UV,these compounds were elucidated by the comparison with spectroscopic data analysis.Among them,compound 1-5,23,45 and 51 are new compounds,fissitungfines A(1)and B(2)were a new type of aporphine related alkaloids,possessing anunprecedented skeleton in which one six-membered carbocyclic ring in classic aporphine alkaloid wasreplaced by one six-membered lactone ring.Compounds 4 and 5 are two unusual aporphine alkaloids with a carboxyl group as a substituent at N-6.And compound 45 represents the first example of a novel naturally occurring morphinandienone alkaloid with a unique cleavage of the C-9-N-17 bond.All of the compound are isolated from Fissistigma tungfangense for the first time.The isolated alkaloids were evaluated for anti-rheumatoid arthritis,antitumor and antibacterial activity.The results of anti-tumor activity showed that compounds 1 and 2 had obvious activities on anti human leukemia cell HL-60,hepatoma carcinoma cell SMMC-7721,A-549,breast cancer cell MCF-7 and colon cancer cell SW480 cell.And the results of antibacterial activity showed that compounds 3,23,24 and 45 exhibited activity against B.subtilis,B.cereus M.tetragenus,S.aureus and E.coli with MIC values of 0.6-5 ?g/m L.Compounds 4 and 5 exhibited activity against B.subtilis,S.aureus and E.coli with MIC values of 5.0-10.0 ?g/mL.