| Summary: | 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-Blue™ 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 dose-dependent 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. Western blotting suggested that ZR-75-1 and Colo-205 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. Keywords: Terminalia bellerica, Anti-cancer activity, UPLC-ESI-MSn, CellTiter-blue
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