Inhibitory effect of apatinib on HL-60 cell proliferation and its mechanism / 南方医科大学学报
Journal of Southern Medical University
;
(12): 871-874, 2011.
Article
in Chinese
| WPRIM
| ID: wpr-332529
ABSTRACT
<p><b>OBJECTIVE</b>To investigate the effect of apatinib, a small-molecule vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, on the proliferation of human acute myeloid leukemia HL-60 cells and explore the possible mechanism.</p><p><b>METHODS</b>MTT assay was used to assess the cytotoxicity of apatinib in HL-60 cells. The apoptosis and cell cycle changes of the cells in response to apatinib treatment were analyzed by flow cytometry, and Western blotting was used to assay P-Akt and P-Erk1/2 expressions in the cells.</p><p><b>RESULTS</b>Apatinib significantly inhibited the proliferation of HL-60 cells in vitro with an IC(50) of 4.96∓0.32 µmol/L. Apatinib treatment significantly increased the apoptotic rate of the cells in a dose-dependent manner, but produced no significant effect on the cell cycle (P>0.05). Western blotting showed that the expressions of P-Akt and P-Erk1/2 decreased in HL-60 cells after a 48-h apatinib treatment.</p><p><b>CONCLUSION</b>Apatinib inhibits the proliferation of HL-60 cells by inducing cell apoptosis probably through the mechanism of inhibiting the expressions of the Akt/Erk1/2 signal transduction pathway.</p>
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Pharmacology
/
Pyridines
/
Protein-Tyrosine Kinases
/
Chemistry
/
Apoptosis
/
HL-60 Cells
/
Cell Proliferation
Limits:
Humans
Language:
Chinese
Journal:
Journal of Southern Medical University
Year:
2011
Type:
Article
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