A Synthetic Naphthochalcone, 2-Hydroxy-2,3,4-trimethoxy-5,6-naphthochalcone, Triggers Caspase-dependent Apoptosis in HCT116 Human Colon Cancer Cells

作者：Lee Mi So; Ahn Seunghyun; Lee Da Hyun; Lee Da Young; Koh Dongsoo; Shin Soon Young^*

来源：Journal of the Korean Society for Applied Biological Chemistry, 2014, 57(6): 769-773.

DOI：10.1007/s13765-014-4294-7

• apoptosis
• caspase
• flavonoids
• naphthochalcone

A novel synthetic naphthochalcone, 2%26apos;-hydroxy-2,3,4-trimethoxy-5%26apos;,6%26apos;-naphthochalcone (HTN), was evaluated for its antitumor activity. The clonogenicity of both Capan-1 pancreatic and HCT116 colon cancer cells was reduced by HTN treatment. Flow cytometry assay showed that HTN induced cell cycle arrest at the G2/M phase at 24 h of treatment and then accumulated sub-G0/G1 phase population at 48 h post-treatment in HCT116 cells. Furthermore, HTN stimulated the cleavages of caspase-9, caspase-7, and poly(ADP-ribose) polymerase (PARP), suggesting that HTN triggers apoptotic cell death through a mitochondria-mediated caspase-dependent pathway. These results suggest that methoxylated naphthochalcone may have a potential as a drug candidate for the treatment of human colon cancer.

• 出版日期2014-12