Li Xing-Qi, Ouyang Zhi-Gang, Zhang Sheng-Hua, Liu Hong, Shang Yue, Li Yi, Zhen Yong-Su
College of Life Science and Technology, Heilongjiang Bayi Agricultural University, Daqing, 163319, China.
J Neurooncol. 2014 Aug;119(1):91-100. doi: 10.1007/s11060-014-1477-3. Epub 2014 May 20.
The present work evaluated the synergistic efficacy of an enediyne antibiotic lidamycin (LDM) plus temozolomide (TMZ) against glioma in vitro and in vivo. LDM plus TMZ inhibited the proliferations of rat glioma C6 cells and human glioma U87 cells more efficiently than the single usage of LDM or TMZ. In addition, LDM also potentiated the apoptosis inductions by TMZ in rat C6 cells and human U87 cells. Meanwhile, the results of TdT-mediated dUTP Nick End Labeling assay for subcutaneous U87 tumor sections indicated an enhanced apoptosis induction in vivo by LDM plus TMZ, which confirmed the high potency of the combination for glioma therapy. As determined by Western blot, apoptosis signal pathways in C6 cells and U87 cells were markedly affected by the synergistic alteration of P53, bax, procaspase 3, and bcd-2 expression. In both subcutaneous U87 xenograft and C6 intracerebral orthotopic implant model, TMZ-induced glioma growth suppression was dramatically potentiated by LDM. As shown, the combination therapy efficiently reduced the tumor volumes and tumor weights of the human glioma U87 xenograft. Kaplan-Meier assay revealed that LDM plus TMZ dramatically prolonged the life span of C6 intracerebral tumor-bearing rats with decreased tumor size. This study indicates that the combination of LDM with TMZ might be a promising strategy for glioma therapy.
本研究评估了烯二炔类抗生素力达霉素(LDM)联合替莫唑胺(TMZ)在体外和体内对胶质瘤的协同疗效。LDM联合TMZ比单独使用LDM或TMZ更有效地抑制大鼠胶质瘤C6细胞和人胶质瘤U87细胞的增殖。此外,LDM还增强了TMZ对大鼠C6细胞和人U87细胞的凋亡诱导作用。同时,对皮下U87肿瘤切片进行TdT介导的dUTP缺口末端标记分析结果表明,LDM联合TMZ在体内增强了凋亡诱导作用,这证实了该联合用药对胶质瘤治疗的高效性。通过蛋白质印迹法测定,C6细胞和U87细胞中的凋亡信号通路因P53、bax、procaspase 3和bcd-2表达的协同改变而受到显著影响。在皮下U87异种移植模型和C6脑内原位植入模型中,LDM均显著增强了TMZ对胶质瘤生长的抑制作用。如图所示,联合治疗有效降低了人胶质瘤U87异种移植瘤的体积和重量。Kaplan-Meier分析显示,LDM联合TMZ显著延长了脑内接种C6肿瘤大鼠的生存期,且肿瘤大小减小。本研究表明,LDM与TMZ联合应用可能是一种有前景的胶质瘤治疗策略。