Preparative purification of anti-tumor derivatives of honokiol by high-speed counter-current chromatography.

摘要: In our program to synthesize a series of novel derivatives as potential analogs honokiol for anti-tumor treatment, we have found that at least three the showed more potency inhibit proliferation K562 leukemia cells and SPC-A1 adenocarcinoma cells. As critical step further synthesis honokiol, composed two isomers one compound with formyl groups, which were hardly separated by common purification methods, needed be rapidly purified. The present work describes analytical preparative high-speed counter-current chromatography (HSCCC) isolation these C-formylation named 3'-formylhonokiol, 5-formylhonokiol 3',5-diformylhonokiol, respectively. solvent system HSCCC separation was hexane-ethyl acetate-methanol-water ratio 1:0.4:1:0.4 (v/v). one-step produced 157.8 mg, 121.6 mg 21.2 5-formylhonokiol, 3',5-diformylhonokiol from crude sample 400mg purities 98.6%, 99.2% 99.6%, respectively, in an elution time 2.5 h. structural identification determined HPLC, (1)H NMR, (13)C NMR mass spectroscopy. Their anti-proliferation effects on K562, A549 cell lines evaluated MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay.