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Induction of apoptosis by esculetin in human leukemia cells.

Abstract
Esculetin, a coumarin compound, has been shown to exhibit antioxidant and anti-inflammatory effects. In the present study, esculetin was found to inhibit the survival of human promyelocytic leukemia HL-60 cells in a concentration-dependent and time-dependent manner. HL-60 cells underwent internucleosomal DNA fragmentation and morphological changes characteristic of apoptosis after a 24-h treatment with esculetin (100 microM). Flow cytometric analysis showed that the hypodiploid nuclei of HL-60 cells were increased to 40.93% after a 36-h treatment with esculetin (100 microM). Further investigation showed that esculetin induced the release of cytochrome c from mitochondria into cytosol in a time-dependent and concentration-dependent manner. Moreover, esculetin application reduced Bcl-2 protein expression to 58% after 9 h as compared with that time at 0. Cysteine protease 32 kDa proenzyme (CPP32), a caspase 3, was activated and its substrate, poly (adenosine diphosphate-ribose) polymerase, was cleaved after a 24-h treatment of HL-60 cells with esculetin. These data suggest that esculetin induces apoptosis in human leukemia cells by increasing cytosolic translocation of cytochrome c and activation of CPP32.
AuthorsC Y Chu, Y Y Tsai, C J Wang, W L Lin, T H Tseng
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 416 Issue 1-2 Pg. 25-32 (Mar 23 2001) ISSN: 0014-2999 [Print] Netherlands
PMID11282109 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antioxidants
  • Cytochrome c Group
  • Proto-Oncogene Proteins c-bcl-2
  • Umbelliferones
  • Poly(ADP-ribose) Polymerases
  • CASP3 protein, human
  • Caspase 3
  • Caspases
  • esculetin
Topics
  • Antioxidants (pharmacology)
  • Apoptosis (drug effects)
  • Caspase 3
  • Caspases (drug effects, metabolism)
  • Cell Survival (drug effects)
  • Cytochrome c Group (drug effects, metabolism)
  • DNA Fragmentation (drug effects)
  • Dose-Response Relationship, Drug
  • HL-60 Cells (cytology, drug effects, metabolism)
  • Humans
  • Poly(ADP-ribose) Polymerases (drug effects, metabolism)
  • Proto-Oncogene Proteins c-bcl-2 (drug effects, metabolism)
  • Time Factors
  • Umbelliferones (pharmacology)

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