Induction of apoptosis and down-regulation of Bcl-XL in cancer cells by a novel small molecule, 2[[3-(2,3-dichlorophenoxy)propyl]amino]ethanol

In a search for new Anticancer agents, we identified that 2[[3-(2,3-dichlorophenoxy) propyl]amino]ethanol (2,3-DCPE) induced Apoptosis more effectively in various Cancer cells than in normal human fibroblasts. We further evaluated the cell-killing effects of this compound in vitro in several human Cancer cell lines and normal human fibroblasts. A cell viability assay showed that IC(50)s for human colon Cancer cell lines LoVo and DLD-1, for human lung Cancer cell lines H1299 and A549, and for normal human fibroblasts were 0.89, 1.95, 2.24, 2.69, and 12.6 micro M, respectively. Subsequent studies revealed that 2,3-DCPE could cause cleavage of Caspase-8, Caspase-3, caspase-9, and poly(ADP-ribose) polymerase and release of cytochrome c in Cancer cells but not in normal human fibroblasts. Our data also showed that 2,3-DCPE attenuated the protein level of Bcl-xL and that Apoptosis induction by 2,3-DCPE could be blocked by enforced overexpression of Bcl-xL. Our results suggest that 2,3-DCPE might be a potential new Anticancer agent.