Chemical Constituents From The Branches And Leaves Of Illicium Wardiiand Anti-bacterial And Anti-tumor Activity

Illicium wardii A. C. Smith belongs to the Illicium genus of the Illiciaceae family. Only one I. genus in the Illiciaceae family, which is evergreen trees or shrubs, is contained 50 species in total in the world and mainly distributed in the north of the earth. While about 28 species and 2 variants of the I. genus in China discovered, most of them are distributed in the southwest, south and east of China, the 21 species of which are uniquely distributed in China.Although there exist many reports about the chemical constituents and bioactivity of Illicium genus, investigations on I. wardii were rarely reported, because of the limited distribution. The research focus on studying the continents from the branches and leaves of the I. wardii, which was obtained from the Gongshan county of Nujiang city, in Yunnan province. Detailed investigation on the branches and leaves of I. wardii led to the isolation of 50 compounds by various chromatographic methods(silica gel column chromatography, Sephadex LH?20 column chromatography, preparative TLC, preparative HPLC, etc.), and their structures were identified on the basis of spectroscopic analysis((ESI?MS, 1H?NMR, 13C?NMR, DEPT, HMQC, HSQC, 1H?1H COSY, HMBC, and NOESY, etc.). The structures of these compounds were identified as 21 lignanoids, 3 terpenoids, 7 flavonoids, 2 anthraquinones, 9 organic acids, 6 aromatic compounds and 2 other compounds. Among them, compounds GS?9, GS?11, GS?25, GS?26, GS?35, GS?36, GS?48 were new dihydrobenzofuran lignans. GS?27 was a new aromatic compound, and GS?32 were a new anthraquinone. Among the known compounds, 46 compounds were isolated from I. wardii for the first time, and 18 compounds of which were obtained from the I. genus for the first time.Fifty compounds were tested for antimicrobial activity against ten bacterias using a microbroth dilution method. Only compounds GS?4, GS?20, GS?45 and GS?27 showed moderate activity against the ten bacterias, respectively.Twenty?five compounds were tested for cytotoxicity against four tumor cell lines using MTT assay. Among them, most of the benzofuran lignanoids show no cytotoxicity against the tumor cell line. Compounds GS?4, GS?20, GS?45 and GS?27 showed significant cytotoxicity against the A549, HCT116, SKOV3 and HepG2. Compounds GS?35, GS?36, GS?42 and GS?13 showed significant cytotoxicity against SKOV3. The structure?activity relationships were concluded, according to their structural features, and the result could provide valuable data for pharmacological studies with the aim of obtaining some cytotoxic compounds that are more selective and potent toward cancer cells.