Studies On The Anti-tumor Constituents Of The Traditional Chinese Medicine Marine Alga, Sargassum Pallidum (Turn.) C.Ag.

Chinese traditional medicine (CTM) plays a very important role in the history of medicine. The research on the effective components of CTM influences the modernization of CTM. Studies have been carried out in our group to investigate the potential anti-tumor compounds derived from marine alga, Sargassum pallidum (Turn.) C. Ag. This dissertation describes the discovery of several anti-tumor lead compounds screened by using brine shrimp and a mouse cdc2 mutant cell line, tsFT210. Studies include bioassay-guided fractionation for compounds with anti-tumor activities, structural elucidation and preliminary evaluation for anti-tumor activities of pure compounds.The ethanol-water extract of S. pallidum was partitioned between water and cyclohexane, ethyl acetate and n-butanol, successively. From the bioactive part, eighteen compounds 1¹8 were isolated by repeated column chromatography on silica gel, Sephadex LH-20 and RP-18, followed by reverse-phase high performance liquid chromatography. By means of spectroscopic method including IR, MS, 1D-NMR, 2D-NMR and their physicochemical properties, the structures of compounds 1¹4 were elucidated as Aurantiamide (1), Benzoylphenylalaninol (2), Thymidine (3), Ficusic acid (4), Bis(2-methylpropyl) ester (5), 4-Hydroxyphthalide (6), 2-Amino-3-phenylbutanoic ester (7), 4(1H)-Quinolinone (8), 2-Cyclohexene-1-acetic acid, 2,6,6-trimethyl-4-oxo- (9), 2-Cyclohexene-1-acetic acid, 2,6,6-trimethyl-4-oxo-, methyl ester (10), 2-Benzothiazolol (11), 2',5-Dihydroxy-6,6',7,8-tetramethoxyflavone (12), 5,6-Dihydroxy-7-methoxyflavone (13), and 5,7-Dihydroxy-8-methoxyflavone (14) .Preliminary evaluation for anti-tumor activities of the pure compounds indicated that compound 3, 6 and 12 showed a tender bioactivity in inhibiting the cell progression at the G₀/G₁ phase of P388 cells; compound 8 and 12 showed a tender bioactivity in the cell progression at the G0/G1 phase of K562 cells; compound 3 possessed tender cytoclasis activity on tsFT210 celles. Compound 3, 6, 8, and 12 are the main compounds with anti-tumor activities in this herb.