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Objective:To investigate the biochemical constituents of the fruits of Terminalia bellerica (Gaertn.) Roxb.(hereafter termed T.bellerica) and estimate the anti-cancer activity of different polar extracts.Methods:To rapidly screen and identify the biochemical constituents of ethyl acetate (EA) extracts of T.bellerica,ultra performance liquid chromatography-electrospray ionization/mass spectrometry (UPLC-ESI-MSn) was done.The CellTiter-BlueTM cell-viability assay was used to ascertain the anti-cancer activity of different polar extracts in 10 human cancer cell lines.Results:Forty polyphenols of the EA extract of T.bellerica were characterized tentatively.The EA extract exhibited significant anti-cancer activity against ZR-75-1 cells (half-maximal inhibitory concentration =27.33 (0.98) μg/mL) and Colo-205 cells (39.65 (2.99) μg/mL) in vitro.Treatment of ZR-75-1 cells with 20 and 60 μg/mL of the EA extract elicited dosedependent apoptosis percentages at an early stage of 17.58 (0.74) ％ and at a late stage of 29.20 (1.22) ％;Colo-205 cells at the same concentration of EA extract had values of 21.33 (1.03) ％ and 40.55 (0.34) ％,respectively.West blotting suggested that ZR-75-1 and Colo205 cells treated with the EA extract showed a similar increasing tendency for expression of cleaved anti-poly adenosine diphosphate ribose polymerase I.Conclusion:We identified a total of 40 chemical constituents,of which 11 were first obtained from the Terminalia Linn.genus using UPLC-ESI-MSn.Meanwhile,we observe that the EA extract of T.bellerica possesses anti-cancer activity,especially against breast and colon cancers.