3-溴丙酮酸抑制肿瘤糖酵解和促进细胞凋亡  

3-bromopyruvate inhibites of tumor glycolysis and promotion of apoptosis

作　　者：潘建民 罗小辉 杨成 肖旺发 李其尚 张晓东[1] PAN Jianmin;LUO Xiaohui;YANG Cheng;XIAO Wangfa;LI Qishang;ZHANG Xiaodong(Department of Gastrointestinal Glandular Surgery,The First Affiliated Hospital of Guangxi Medical University,Nanning 530000,China)

机构地区：[1]广西医科大学第一附属医院胃肠腺体外科,南宁530000

出　　处：《生命的化学》2022年第8期1461-1469,共9页Chemistry of Life

基　　金：国家自然科学基金项目(81760476)。

摘　　要：肿瘤细胞的生长所需的能量主要来自糖酵解产生的三磷酸腺苷(adenosine triphosphate,ATP)。基于该理论,国内外大量研究者对肿瘤能量代谢相关靶点展开研究。近年来不断有研究指出,3-溴丙酮酸(3-bromopyruvate,3-BrPA)作为一种烷化剂,具有抗肿瘤作用,其机制可能是对糖酵解关键酶起到抑制作用,从而阻断肿瘤的能量来源、诱导活性氧产生,最终促进肿瘤细胞凋亡,且对肿瘤周围的组织器官没有影响;也有相关研究发现:3-BrPA可逆转肿瘤细胞耐药性、增强光敏剂疗效和提高肿瘤细胞对抗癌药物敏感性。因此,3-BrPA有望成为一种高效、低毒的抗肿瘤药物。本文通过调研国内外关于3-BrPA相关实验的研究,对3-BrPA抑制肿瘤细胞糖代谢和促进肿瘤细胞凋亡的可能机制进行探讨,以期为抗肿瘤药物研究提供一定帮助。Considering that the energy required for tumor cell growth mainly comes from adenosine triphosphate(ATP)produced by the aerobic glycolysis,various investigations have been carried out on tumor energy metabolism related targets.In recent years,3-bromopyruvate(3-BrPA),a strong alkylating agent,has been reported to have anti-tumor effects.The mechanism may be to inhibit the key enzymes of glycolysis,so as to block the energy source of tumor,which induces the production of reactive oxygen species,and finally leads to the apoptosis of tumor cells without affecting the tissues and organs around the tumor.Moreover,some studies have reported that 3-BrPA reversed tumor cell drug resistance,enhanced the efficacy of photosensitizers and improved the sensitivity of tumor cells to anticancer drugs.Therefore,3-BrPA is expected to be a highly efficient anti-tumor agent with low-toxicity.In this paper,based on our investigations and researches on studies concerning 3-BrPA at home and aboard,we discussed the possible mechanism of 3-BrPA in terms of inhibiting glucose metabolism of tumor cells and promoting tumor cell apoptosis,in the hope of providing some help for the study of anti-tumor drugs.

关 键 词：3-溴丙酮酸 糖酵解 己糖激酶 活性氧 凋亡 

分 类 号：R730.2[医药卫生—肿瘤]