[Apoptotic mechanism of WJH-6, a novel polyamine conjugate, on K562 and HL-60 cells].

In the present study,the apoptotic mechanism and polyamine transporter recognition of WJH-6,a novel polyamine conjugate,were investigated in K562 and HL-60 cells. The cytotoxicity of WJH-6 was assessed by MTT assay; cell cycle distribution and apoptosis were measured by flow cytometry; the protein expression of Caspase-3,Caspase-8,Caspase-9,Bid and mitochondrial membrane potential (MMP) were evaluated by high content screening (HCS) analysis; the protein expression of cytochrome c was measured by Western blotting. The results showed that WJH-6 could be recognized and transported by polyamine transporter (PAT). Furthermore,WJH-6 was able to inhibit K562 and HL-60 cells proliferation and induce apoptosis. This apoptotic effect was relative to MMP loss,cytochrome c release from mitochondria to cytoplasm and the activation of Caspase-8,Caspase-9,Caspase-3 and Bid. These results suggested that WJH-6-induced K562 and HL-60 cells apoptosis was related with mitochondrial damage.