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Isochamaejasmin induces apoptosis in leukemia cells through inhibiting Bcl-2 family proteins

  • Shou De Zhang
  • , Lei Shan
  • , Wei Li
  • , Hong Lin Li*
  • , Wei Dong Zhang
  • *Corresponding author for this work
  • East China University of Science and Technology
  • Naval Medical University
  • Qinghai Academy of Agriculture and Forestry Science

Research output: Contribution to journal › Article › peer-review

Abstract

The biflavonoid isochamaejasmin is mainly distributed in the root of Stellera chamaejasme L. (Thymelaeaceae) that is used in traditional Chinese medicine (TCM) to treat tumors, tuberculosis, and psoriasis. Herein, isochamaejasmin was found to show similar bioactivity against Bcl-2 family proteins to the reference Bcl-2 ligand (-)-gossypol through 3D similarity search. It selectively bound to Bcl-xl and Mcl-1 with Ki values being 1.93 ± 0.13 μmol·L-1 and 9.98 ± 0.21 μmol·L-1, respectively. In addition, isochamaejasmin showed slight growth inhibitory activity against HL-60 with IC50 value being 50.40 ± 1.21 μmol·L-1 and moderate growth inhibitory activity against K562 cells with IC50 value being 24.51 ± 1.62 μmol·L-1. Furthermore, isochamaejasmin induced apoptosis of K562 cells by increasing the intracellular expression levels of proteins of the cleavage of caspase-9, caspase-3, and PARP which involved in the Bcl-2-induced apoptosis pathway. These results indicated that isochamaejasmin induces apoptosis in leukemia cells by inhibiting the activity of Bcl-2 family proteins, providing evidence for further studying the underlying anti-cancer mechanism of S. chamaejasme L.

Original languageEnglish
Pages (from-to)660-666
Number of pages7
JournalChinese Journal of Natural Medicines
Volume13
Issue number9
DOIs
StatePublished - 1 Sep 2015
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

Keywords

  • (-)-Gossypol
  • 3D Similarity search
  • Apoptosis
  • Bcl-2
  • Isochamaejasmin
  • Stellera chamaejasme L.

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