Apatinib Suppresses Proliferation and Induced Apoptosis of Human Breast Cancer Cell Line MDA-MB-231 Through Glycolytic Inhibition

Objective To investigate the antitumor effect of apatinib on breast cancer cells in vitro and its mechanism.

Methods CCK-8 assay was used to detect the inhibitory effect of apatinib on the proliferation of breast cancer cell line MDA-MB-231. Annexin V-FITC/PI apoptosis detection kit was used to detect the effect of apatinib on the apoptosis of MDA-MB-231 cells. The effect of apatinib on lactate production in MDA-MB-231 cells was detected by lactate content assay kit. The effect of apatinib on the extracellular acidification rate of MDA-MB-231 cells was detected by glycolysis stress test kit.

Results Apatinib inhibited the proliferation of breast cancer MDA-MB-231 cells in vitro in a concentration-dependent manner (P < 0.05). The half maximal inhibitory concentration (IC₅₀) of apatinib in MDA-MB-231 cells was 1.56μmol/L for 48h treatment. Apatinib also induced the apoptosis of MDA-MB-231 cells in a concentration-dependent manner (P < 0.05). Apatinib inhibited intracellular lactate content in MDA-MB-231 cells in a concentration-dependent manner (P < 0.05). Apatinib also decreased extracellular acidification rate of MDA-MB-231 cells, including glycolytic capacity and glycolytic reserve (P < 0.05).

Conclusion Apatinib could induce the apoptosis of breast cancer cell line MDA-MB-231 by inhibiting aerobic glycolysis.