Chalcone HTMC causes in vitro selective cytotoxicity, cell-cycle G1 phase arrest through p53-dependent pathway in human lung adenocarcinoma A549 cells, and in vivo tumor growth suppression

Chalcone derivative 2′-hydroxy-2,3,4′,6′-tetramethoxychalcone (HTMC) inhibited the growth of human lung cancer cell lines without cytotoxic to normal cells. In A549 lung adenocarcinoma cells, HTMC caused G1 phase cell-cycle arrest, inhibited the cell-cycle regulatory proteins phosphorylation of cdc2 (Tyr15 and Tyr161) and Rb (Ser795 and Ser807/811), and accumulated the tumor suppresser genes p53 and p21. In addition, in vivo data demonstrated that HTMC act as a tumor growth suppressing agent.