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To explore the cancer cells inhibitory constituents in Aquilaria sinensis leaves, a new food raw material, applying bioassay-guided method by using cytotoxicity test to three human cancer cell lines, cancer cells inhibitory activity of different polar fractions extracted from wild and cultivated A. sinensis leaves by different solvents and twelve monomeric compounds were tested. It is disclosed that, cancer cells cytotoxicity of different polar fractions from wild A. sinensis leaves were better than that from cultivated A. sinensis leaves, no matter in what solvent extraction. The better cancer cells cytotoxicity lied in petroleum ether and ethyl acetate fraction extracted by 70% acetone from wild A. sinensis leaves, with the IC50 value low to 9.09±0.93 and 10.65±1.52 μg/mL to DU145 cell line. Twelve compounds were isolated though the bioassay-guided method, eleven of which exhibited slight to moderate inhibitory activities against human prostate cancer cell lines (PC-3 or DU145), while two compounds also exhibited moderate inhibitory activities against human hepatocellular cancer cell lines (HepG2). The best cancer cells cytotoxicity lied in Compound 9 with the IC50 value low to 11.05±2.04 μM to DU145 cell line.

Bioassay-guided Separation of Cancer Cells Inhibitory Constituents in <em>Aquilaria sinensis</em> Leaves: A New Food Raw Material