Wagenblast Jens, Hirth Daniel, Thron Laura, Arnoldner Christoph, Diensthuber Marc, Stöver Timo, Hambek Markus
ENT Department, Medical School, Goethe University, D-60590 Frankfurt am Main, Germany.
Oncol Lett. 2012 Jul;4(1):175-177. doi: 10.3892/ol.2012.700. Epub 2012 Apr 30.
Inhibition of the Polo-like-kinase-1 (PLK1) has been shown to be effective in a number of solid tumor models. In this in vitro study, we examined the antitumor effect of BI2536, a small molecule inhibitor of PLK1, in squamous cell carcinoma of the head and neck (SCCHN) cell lines. Dose escalation studies were performed with nine SCCHN cell lines using BI2536. Growth inhibitory and proapoptotic effects were measured quantitatively using cytohistology and a Human Apoptosis Array Kit. BI2536 demonstrated a significant antiproliferative and apoptotic activity in all nine SCCHN cell lines investigated (p<0.009). Our results indicate that inhibition of PLK1 by BI2536 leads to an antiproliferative and apoptotic effect in SCCHN cell lines. In vivo and in the clinical setting, the application of BI2536 may support the antitumoral activity of conventional drugs that are in current use and could decrease the systemic toxicity of these drugs.
在多种实体瘤模型中，抑制Polo样激酶-1（PLK1）已显示出有效性。在这项体外研究中，我们检测了PLK1小分子抑制剂BI2536对头颈部鳞状细胞癌（SCCHN）细胞系的抗肿瘤作用。使用BI2536对9种SCCHN细胞系进行了剂量递增研究。采用细胞组织学和人凋亡阵列试剂盒定量测定生长抑制和促凋亡作用。在所有研究的9种SCCHN细胞系中，BI2536均表现出显著的抗增殖和凋亡活性（p<0.009）。我们的结果表明，BI2536抑制PLK1可导致SCCHN细胞系出现抗增殖和凋亡效应。在体内和临床环境中，应用BI2536可能会增强目前正在使用的传统药物的抗肿瘤活性，并降低这些药物的全身毒性。
