Studies On The Consitituents And Antitumor Activity Of Lindera Aggregata (SIMS) Kosterm

Based on the review on the chemical constituents and pharmacological research of Lindera aggregata (Sims) Kosterm., the chemical constituents of the alcohol extract were investaged and their antitumor activities were evaluated.The dried and shattered roots of L. aggregate were extracted with 95%EtOH by percolation. Then the extract was extracted by petroleum ether, ethyl acetate, n-butanol, to divide into three parts. The petroleum ether and ethyl acetate solubles were separated preliminary with silica gel chromatographic methods. Then, various chromatographic methods such as silica gel, Sephadex LH-20, RP-C18 column chromatography, recrystallization and semi-preparative HPLC were used over and over again to separate and purify the compounds. Finally, twenty compounds have been isolated.Fifteen compounds of them which had been identified were elucidated by TLC,*H NMR, 13C NMR, HR-ESI-MS, HSQC, COSY, HMBC, ROSEY and compared with the known compounds. Among the total,β-sitosterol (4) is a steroid,5-styrylfuran-2-carboxylic acid methyl ester (12) is a benzene derivatives, the last thirteen compounds are sesquiterpenes, they were identified as:linderane (1), linderalactone (2), hydroxylinderstrenolide (3), pseudoneolinderane (5), dehydrolindestrenolide (6), (+)-linderadine (7), lindenanolide A (8), strychnistenolide C (9),6a-acetyllindenanolide B1 (10),6a-acetyllindenanolide B2 (11), lindenanolide I (13), linderanine-C (14), (-)-hydroxylinderastrenolide (15). These sesquiterpenes contain six germacranes (1,2,5,7,14), three eudesmanes (3,6,15), four lindenranes (8,9,10,11) and one guaiane (13). By searching data-base of SciFinder Scholar, compound 13 is identified as new compound and compound 9 is identified as new natural product. And compounds 9,12,13,15 were isolated from the plant for the first time.In addition, the cytotoxicity activities of the compounds 1,2,3,5,6 were tested against MDA-MB-231 cancer cell lines by CCK.-8 in vitro. However, the compounds showed no cytotoxicity. Then the cytotoxicity activities of the compounds 2,3,5,6,7 were evaluated against HT-29 cancer cell lines by MTT in vitro. The eudesmanes 3,6 (IC50:33.35,57.89 μg/mL) showed stronger cytotoxicity than the germacranes 2,5,7 ((IC50:153.18,143.87, 193.12μg/mL).