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学科主题: 临床医学
题名:
3-Bromopyruvic Acid, A Hexokinase II Inhibitor, is an Effective Antitumor Agent on the Hepatoma Cells: in vitro and in vivo Findings
作者: Gong, Lei1,2; Wei, Yuhua1; Yu, Xin1; Peng, Jirun1; Leng, Xisheng1
关键词: Antitumor effect ; 3-Bromopyruvic acid ; hepatoma BEL-7402 cells ; Hexokinase II
刊名: ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
发表日期: 2014-06-01
卷: 14, 期:5, 页:771-776
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Oncology ; Chemistry, Medicinal
研究领域[WOS]: Oncology ; Pharmacology & Pharmacy
关键词[WOS]: TARGETING CANCER METABOLISM ; HEPATOCELLULAR-CARCINOMA ; GLUCOSE-METABOLISM ; LIVER-TUMOR ; MODEL ; GLYCOLYSIS ; APOPTOSIS ; EFFICACY ; THERAPY ; WARBURG
英文摘要:

Over-expressed in cancer cells, hexokinase II (HK II) forms a mitochondrial complex, which promotes cancer survival. 3-Bromopyruvic acid (3-BrPA) dissociates HK II from this complex, causing cell death, and thus, having an anti-tumor effect. The design of this study was to first analyze the expression of HK II in the hepatoma cell line, BEL-7402, then investigate the effects of 3-Br-PA on these cells, and finally, discuss its potential for clinical usage. HK II expression was detected in BEL-7402 cells by immunocytochemistry and reverse transcriptase polymerase chain reaction (RT-PCR). In vitro treatment of cells with 3-BrPA significantly inhibited their growth, as evaluated by MTT assay and adenosine triphosphate-tumor chemosensitivity assay (ATP-TCA). To analyze the in vivo function and safety of this drug, a tumor model was established by subcutaneously implanting hepatic cancer cells into nude mice. 3-BrPA treatment (50 mg/kg ip. daily, 6 days/week for three weeks) was effective in the animal model by attenuating tumor growth and causing tumor necrosis. Toxic signs were not observed. The acute toxicity study provided an LD50 of 191.7 mg/kg for 3-BrPA. Taken together, our in vitro and in vivo analyses suggest that 3-BrPA exerts anti-hepatoma effects, and may be an effective pharmacological agent for the treatment of hepatocellular carcinoma.

语种: 英语
WOS记录号: WOS:000335390800015
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/63699
Appears in Collections:北京大学第二临床医学院_肝胆外科_期刊论文

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作者单位: 1.Peking Univ, Dept Hepatobiliary Surg, Peoples Hosp, Beijing 100044, Peoples R China
2.Tsinghua Univ, Dept Gen Surg, Beijing Tsinghua Hosp, Beijing, Peoples R China

Recommended Citation:
Gong, Lei,Wei, Yuhua,Yu, Xin,et al. 3-Bromopyruvic Acid, A Hexokinase II Inhibitor, is an Effective Antitumor Agent on the Hepatoma Cells: in vitro and in vivo Findings[J]. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY,2014,14(5):771-776.
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