Constituents isolated from Glehnia littoralis suppress proliferations of human cancer cells and MMP expression in HT1080 cells

Crude extract and solvent-partitioned fraction of Glehnia littoralis were found to possess different anti-proliferative effects against AGS, HT1080 and U937 human cancer cells. The crude extracts and solvent fractions dose-dependently inhibited cell proliferation. Especially, n-hexane and 85% aqueous MeOH fractions exhibited comparatively higher anti-proliferative effects and reduced expressions of Bcl-2, COX-2 and iNOS genes. Systematic separation of all solvent fractions by chromatographic methods led to the isolation of three glucopyranosides, four furanocoumarins and two polyacetylenic alcohols. All the nine compounds were evaluated for their inhibitory effects against both proliferation of human cancer cells and expressions of MMP-2 and -9 in HT1080 cells. Two polyacetylenic alcohols exerted the highest inhibitory activity against both human cancer cell lines, and MMP-2 and -9. These results suggest that G. littoralis may possibly be used as a valuable chemopreventive agent or food supplement for reducing cancer risk.