Glycolysis inhibitor induces apoptosis of gastric cancer cells by inhibiting glycolysis and promoting mitochondria-regulated pathway

ObjectiveTo investigate the mechanism of glycolysis inhibitor WZB117-induced apoptosis in human gastric cancer cell line MGC-803 by inhibiting glycolysis and promoting mitochondria-regulated apoptotic pathway.

MethodsGastric cancer cell line MGC-803 was used in this study, and exponential growth cells were used in the experiment.According to the experimental requirements, the cultured cells were divided into control group(normally cultured cells) and WZB117 group(cells treated with 20 μg/mL glucose transporter inhibitor).The proliferation of cells was detected by MTS kit.Cell viability was measured by CCK-8 and apoptosis was analyzed by TUNEL.Mitochondrial function was detected by ATP content.The expression of Bcl-2, Bax, caspase-3, Cyt-c and glycolysis-related enzymes cells in hexokinase(HK) and cells in phosphofructokinase(PFK) were analyzed by Western blotting.

ResultsThe proliferation of WZB117 group was lower than that in control group at 24 h and 48 hours(P < 0.01).The apoptosis rate in WZB117 group was higher than that in control group(P < 0.01), and the cell viability in WZB117 group was lower than that in control group(P < 0.01).The ATP content in WZB117 group was lower than that in control group at 12 h and 24 h(P < 0.01).The expression of Bcl-2 protein in WZB117 group was lower than that in control group(P < 0.01), and the expression of Bax, caspase-3 and Cyt-c protein in WZB117 group was higher than that in control group(P < 0.01).The expression of HK and PFK in WZB117 group was lower than that in control group(P < 0.01), indicating that WZB117 could inhibit the expression of enzymes related to glycolysis.

ConclusionsWZB117 induces apoptosis of gastric cancer cell line MGC-803 by inhibiting glycolysis pathways and reducing mitochondrial ATP production.