In order to investigate the potential of Glehnia littoralis as a cancer chemopreventive food, antiproliferative effects of both its crude extracts and solvent-partitioned fractions (n-hexane, 85% aq. MeOH, n-BuOH, and water) were evaluated in HT-29 human colon cancer cells. Its crude extracts and solvent-partitioned fractions exhibited dose-dependent inhibitory effects on the cell proliferation. Especially, n-hexane and 85% aq. MeOH fractions exhibited a high antiproliferative effect, induced apoptosis as determined by 4,6-diamidino-2-phenylindole (DAPI) staining, and reduced mRNA expression of Bcl-2, cyclooxygenase (COX-2) and inducible nitric oxide synthase (iNOS). Systematic separation of n-hexane and 85% aq. MeOH fractions by diverse chromatographic methods led to the isolation of furanocoumarins (1-4) and polyacetylene alcohols (5-7). All compounds exhibited dose-dependent inhibitory effects on the cell proliferation. These results indicated that potent inhibitory activity of G. littoralis on proliferation of cancer cells can be significantly traceable to furanocoumarines and polyacetylenic alcohols contained in G. littoralis. (C) 2009 Elsevier Ltd. All rights reserved.