A methoxyflavanone derivative, 2′,3′,4′-trimethoxy-5,6-naphthoflavanone, inhibits proliferation of HCT116 human colon cancer cells by inducing G2/M cell cycle arrest and apoptosis

Abstract

A methoxylated flavanone derivative, 2′,3′,4′-trimethoxy-5,6-naphthoflavanone (TMNF), was synthesized, and its anti-proliferative activity was evaluated. In HCT116 colon cancer cells, TMNF inhibited cellular proliferation and triggered cytotoxicity. A flow cytometry assay showed that TMNF caused cell cycle arrest at the G2/M phase with a concomitant decrease in the population of G1 phase cells. Furthermore, TMNF caused accumulation of p53 and its downstream target, Bax, and stimulated cleavage of caspase-7 and poly(ADP-ribose) polymerase. These data suggest that methoxylated naphthoflavanone can be an attractive pharmacophore for further development of therapeutic adjuvants.