Butein, a plant polyphenol, induces apoptosis concomitant with increased caspase-3 activity, decreased Bcl-2 expression and increased Bax expression in HL-60 cells

Pharmacol Toxicol. 2001 May;88(5):261-6. doi: 10.1034/j.1600-0773.2001.d01-114.x.


In the present study we have investigated whether butein could induce apoptosis in human leukaemic HL-60 cells. The treatment of HL-60 cells with butein induced apoptotic cell death as determined by morphological and biochemical changes. Apoptotic DNA fragments in the butein-treated HL-60 cells were increased gradually as determined by flow cytometric analysis. The caspase-3 activity was increased during butein-induced apoptosis. However, caspase-3 inhibitor abrogated the butein-induced DNA fragmentation. Furthermore, the treatment of HL-60 cells with butein decreased the expression of Bcl-2 protein, but increased the expression of Bax protein. These results suggest that butein-induced apoptosis is mediated through the activation of caspase-3 and it is associated with changed expression of Bcl-2 and Bax proteins.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis / drug effects*
  • Caspase 3
  • Caspases / metabolism*
  • Cell Survival / drug effects
  • Chalcone / analogs & derivatives*
  • Chalcone / pharmacology*
  • Chalcones
  • DNA Fragmentation / drug effects
  • Dose-Response Relationship, Drug
  • Electrophoresis, Agar Gel
  • Enzyme Activation
  • Enzyme Precursors
  • Flow Cytometry
  • HL-60 Cells
  • HeLa Cells
  • Humans
  • K562 Cells
  • Phosphodiesterase Inhibitors / pharmacology*
  • Ploidies
  • Proto-Oncogene Proteins / metabolism*
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Tumor Cells, Cultured
  • U937 Cells
  • bcl-2-Associated X Protein


  • BAX protein, human
  • Chalcones
  • Enzyme Precursors
  • Phosphodiesterase Inhibitors
  • Proto-Oncogene Proteins
  • Proto-Oncogene Proteins c-bcl-2
  • bcl-2-Associated X Protein
  • butein
  • Chalcone
  • CASP3 protein, human
  • Caspase 3
  • Caspases