Matsuo Taisuke, Konya Yumiko, Hirayama Eri, Sadzuka Yasuyuki
Division of Advanced Pharmaceutics, Department of Clinical Pharmaceutical Sciences, School of Pharmacy, Iwate Medical University, Iwate 028-3694, Japan.
Oncol Lett. 2020 Jul;20(1):962-966. doi: 10.3892/ol.2020.11616. Epub 2020 May 13.
Cancer cells switch from mitochondrial oxidative phosphorylation to glycolysis, even in the presence of normal oxygen concentrations. Inhibition of the glycolytic pathway is therefore a critical strategy in cancer therapy. A non-metabolic glucose analog, 2-deoxy-D-glucose (2-DG), has been the focus of research on glycolytic inhibitors for use in cancer treatment. The current study examined the anti-cancer effects of 2-DG on idarubicin (IDA)-resistant P388 (P388/IDA) leukemia cells. P388/IDA cells were established following continuous exposure of IDA to P388 cells. Characterization of P388/IDA cells revealed increased lactate production and glucose consumption compared with P388 parent cells. The results of a cell viability assay determined that 2-DG induces higher toxicity in P388/IDA cells compared with P388 cells. Although 2-DG also exhibits endoplasmic reticulum (ER) stress-inducing activity, the cytotoxic effect of the ER stress inducer, tunicamycin, on P388/IDA cells was lower than that of P388 cells. A combination of 2-DG and IDA enhanced P388/IDA cell death compared with each agent alone. The results indicated that P388 cells activated glycolysis after acquiring IDA resistance and therefore, inhibition of the glycolytic pathway via 2-DG might be a useful strategy for cancer therapy against IDA- resistant leukemia cells.
癌细胞即使在正常氧浓度下也会从线粒体氧化磷酸化转变为糖酵解。因此,抑制糖酵解途径是癌症治疗中的关键策略。一种非代谢性葡萄糖类似物2-脱氧-D-葡萄糖(2-DG)一直是用于癌症治疗的糖酵解抑制剂研究的焦点。当前研究检测了2-DG对阿糖胞苷(IDA)耐药的P388(P388/IDA)白血病细胞的抗癌作用。P388/IDA细胞是在IDA持续作用于P388细胞后建立的。与P388亲代细胞相比,P388/IDA细胞的特征显示乳酸生成和葡萄糖消耗增加。细胞活力测定结果表明,与P388细胞相比,2-DG对P388/IDA细胞诱导更高的毒性。尽管2-DG也表现出诱导内质网(ER)应激的活性,但ER应激诱导剂衣霉素对P388/IDA细胞的细胞毒性作用低于对P388细胞的作用。与单独使用每种药物相比,2-DG和IDA联合使用可增强P388/IDA细胞死亡。结果表明,P388细胞在获得IDA耐药性后激活了糖酵解,因此,通过2-DG抑制糖酵解途径可能是针对IDA耐药白血病细胞的癌症治疗的有用策略。