Anti-proliferative effects of indomethacin, acemetacin and their tromethamine salts in HCT116 human colon cancer cells

Background and Aims: Since 1980's, several preclinical studies have been published on the anti-colorectal cancer activity of nonsteroidal anti-inflammatory drug indomethacin. The direct anti-proliferative effect indomethacin seems to occur via a variety reported COX-independent mechanisms. Acemetacin is glycolic acid ester derivative contrary indomethacin, there not much research anti-cancer effects acemetacin. Herein, we compared in vitro properties acemetacin, their tromethamine salts HCT116 colon cells. Methods: acemetacin were synthesized structures established by microanalysis, IR, 1 H-NMR, 13C-NMR (APT) 2D-NMR (HSQC HMBC) spectrometry. Cell proliferation assays performed using xCELLigence real-time cell analysis system. Results: Indomethacin exhibited profound inhibitory with IC50 values at low micromolar ranges. far lower cytotoxic as that Surprisingly, indomethacin-tromethamine salt was 2-fold 4.4-fold more potent than 48 72 h, respectively, while maintaining its 24 h. h post-treatment. Conclusion: cells found be micro-molar levels. esterification caused strong decrease effect. formation positive may promising candidate for additional vivo studies.