| The roots of Platycodon grandiflorum (Jacq.) A. DC. have been extensively used in TCM, called "Jiegeng" (Japanese name: Kikyo) for the treatment of cough and pectoral diseases. Although a lot of studies on chemistry and pharmacology of Platycodon were reported, the research on the antitumor principles of the medicine was not reported. In order to exploit the plant resource and find new antitumor compounds, the study on the constituents of Jiegeng was carried out.From the roots of Platycodon grandiflorum, 21 constituents were isolated by various chromatographic methods, such as silica gel C. C., Sephadex LH-20 C. C., MPLC and HPLC. On the basis of UV, IR, NMR, MS data, measurement of physico-chemical characters and chemical methods, the structures of 15 compounds were identified as 3 triterpenoid saponins, 3 steroids, 4 fructosides, 2 compounds with long chains, and 3 other types. Among them, a new natural compound is 3-O-β-laminari -biosyl-2β, 3β, 16α, 23-tetrahydroxyolean-12-ene-28-oic acid (1). Compound 3 is determined as 3-O-β-D-xylopyranosyl-(1→4)-β-D-glucopyranosyl-2β,3β,16α-trihydro-xyolean-12-ene-28-oic acid 28-O-β-D-apiopyranosyl-(1→3)-β-D-xylopyranosyl-(1→4) -α-L-rhamnopyranosyl-(1→2)-α-L-arabinopyranoside, which has not been reported in the literature.The known compounds are platycodin D (2), spinasterol (4),Δ7-stigmasterol (5), daucosterol (6), n-butyl-O-β-D-fructopyranoside (7), methyl-O-α-D-fructofuranoside (8), methyl-O-β-D-fructofuranoside (9), D-fructose (10), D-glucitol (11), 5-hydroxymethylfurfural (12),α-tocopherol (13), glycerylα-monopalmitate (14) and L-glutamic acid (15). Among them, compound 6-9,11-13 were isolated from this genus for the first time.The ethanol extract and the petroleum ether, CHCl3, EtOAc and n-BuOH fraction, the isolated compounds were tested for their inhibitory activity against MCF-7 and HL-60 tumor cell lines by MTT method. The compound 2 (Platycodin D) showed significant inhibition against the two tumor cells.
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