title: 3-Bromopyruvate inhibits human gastric cancer tumor growth in nude mice via the inhibition of glycolysis.
abstract: Tumor cells primarily depend upon glycolysis in order to gain energy. Therefore, the inhibition of glycolysis may inhibit tumor growth. Our previous study demonstrated that 3-bromopyruvate (3-BrPA) inhibited gastric cancer cell proliferationin vitro. However, the ability of 3-BrPA to suppress tumor growthin vivo,and its underlying mechanism, have yet to be elucidated. The aim of the present study was to investigate the inhibitory effect of 3-BrPA in an animal model of gastric cancer. It was identified that 3-BrPA exhibited strong inhibitory effects upon xenograft tumor growth in nude mice. In addition, the antitumor function of 3-BrPA exhibited a dose-effect association, which was similar to that of the chemotherapeutic agent, 5-fluorouracil. Furthermore, 3-BrPA exhibited low toxicity in the blood, liver and kidneys of the nude mice. The present study hypothesized that the inhibitory effect of 3-BrPA is achieved through the inhibition of hexokinase activity, which leads to the downregulation of B-cell lymphoma 2 (Bcl-2) expression, the upregulation of Bcl-2-associated X protein expression and the subsequent activation of caspase-3. These data suggest that 3-BrPA may be a novel therapy for the treatment of gastric cancer.
authors.affiliation: Department of Gastrointestinal and Gland Surgery, The First Affiliated Hospital of Guangxi Medical University, Guangxi 530021, P.R. China.
authors.forename: Shu-Lin
authors.initials: SL
authors.lastname: Xian
authors.affiliation: Department of Gastrointestinal and Gland Surgery, The First Affiliated Hospital of Guangxi Medical University, Guangxi 530021, P.R. China.
authors.forename: Wei
authors.initials: W
authors.lastname: Cao
authors.affiliation: Department of Gastrointestinal and Gland Surgery, The First Affiliated Hospital of Guangxi Medical University, Guangxi 530021, P.R. China.
authors.forename: Xiao-Dong
authors.initials: XD
authors.lastname: Zhang
authors.affiliation: Department of Gastrointestinal and Gland Surgery, The First Affiliated Hospital of Guangxi Medical University, Guangxi 530021, P.R. China.
authors.forename: Yun-Fei
authors.initials: YF
authors.lastname: Lu
keywords: 3-bromopyruvate; apoptosis; hexokinase; nude mouse; treatment