Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Effect of AC-264, a Novel Indole Derivative, on Apoptosis in HL-60 Cells

  • Lee, Kyeong (College of Pharmacy, Dongguk University-Seoul) ;
  • Kwon, Ok-Kyoung (Immune Modulator Research Center, Korea Research Institute of Bioscience and Biotechnology) ;
  • Xia, Yan (College of Pharmacy, Dongguk University-Seoul) ;
  • Ahn, Kyung-Seop (Immune Modulator Research Center, Korea Research Institute of Bioscience and Biotechnology)
  • Received : 2010.09.27
  • Accepted : 2010.11.02
  • Published : 2010.12.20
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Abstract

The anticancer effect and apoptotic mechanism of a novel indole derivative AC-264, a lead derived from a chemical library, were investigated in human promyelocytic leukemia HL-60 cells. HL-60 cells treated with AC-264 at various concentrations showed the morphological features of apoptosis, such as plasma membrane blebbing and cell shrinkage. AC-264 exhibited cytotoxic effect in various cancer cell lines with different degrees of potency. Especially, AC-264 was effective on increasing the population of apoptotic cells in HL-60 cells, as detected by the number of cells stained with Annexin V and PI. Furthermore, AC-264 activated caspase-3 enzyme activity and induced internucleosomal DNA fragmentation. These results indicated that AC-264 produces anti-cancer effect via apoptotic cell death by activating caspase-3 and inducing internucleosomal DNA fragmentation in HL-60 cells.

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