POETIC Laboratory for Preclinical and Drug Discovery Studies, University of Calgary, Calgary, Alberta, Canada.
Division of Pediatric Oncology, Alberta Children's Hospital, 2888 Shaganappi Trail NW, Calgary, Alberta, T3B 6A8, Canada.
Invest New Drugs. 2020 Jun;38(3):690-699. doi: 10.1007/s10637-019-00816-1. Epub 2019 Jul 2.
High-risk, relapsed and refractory neuroblastoma are associated with poor 5-years survival rates, demonstrating the need for investigational therapeutic agents to treat this disease. Taurolidine is derived from the aminosulfoacid taurine and has known anti-microbial and anti-inflammatory properties. Taurolidine has also demonstrated anti-neoplastic effects in a range of cancers, providing the rationale to investigate the activity of taurolidine against neuroblastoma in preclinical studies. We investigated the in vitro activity of taurolidine against neuroblastoma using the alamar blue cytotoxicity assay, phase-contrast light microscopy, western blotting and analysis of global gene expression by RNA-Seq. In vivo activity of taurolidine was evaluated using mouse xenograft models. In vitro pre-clinical data show that taurolidine is cytotoxic to neuroblastoma cell lines, inducing cell death by apoptosis. Analysis of global gene expression and determination of signaling pathway activation scores using the in silico Pathway Activation Network Decomposition Analysis (iPANDA) platform indicates that taurolidine has an effect on the Notch, mitogen-activated protein kinase (MAPK) and interleukin-10 (IL-10) signaling pathways. In vivo experiments in xenograft mouse models show that taurolidine decreases tumor growth and improves survival. These results provide supportive pre-clinical data on the activity of taurolidine against neuroblastoma. The findings support the rationale for further evaluation of taurolidine for the treatment of relapsed/refractory neuroblastoma patients in an early phase clinical trial.
高危、复发和难治性神经母细胞瘤的 5 年生存率较差,这表明需要研究治疗药物来治疗这种疾病。牛磺脱氧胆酸来源于氨基磺酸牛磺酸,具有已知的抗菌和抗炎特性。牛磺脱氧胆酸在多种癌症中也表现出抗肿瘤作用,这为研究牛磺脱氧胆酸在临床前研究中对神经母细胞瘤的活性提供了依据。我们使用阿尔玛蓝细胞毒性测定法、相差显微镜、蛋白质印迹和 RNA-Seq 分析全局基因表达来研究牛磺脱氧胆酸对神经母细胞瘤的体外活性。使用小鼠异种移植模型评估牛磺脱氧胆酸的体内活性。体外临床前数据表明,牛磺脱氧胆酸对神经母细胞瘤细胞系具有细胞毒性,通过细胞凋亡诱导细胞死亡。使用计算机化途径激活网络分解分析(iPANDA)平台分析全局基因表达和确定信号通路激活评分表明,牛磺脱氧胆酸对 Notch、丝裂原活化蛋白激酶(MAPK)和白细胞介素 10(IL-10)信号通路有影响。在异种移植小鼠模型中的体内实验表明,牛磺脱氧胆酸可减少肿瘤生长并提高存活率。这些结果为牛磺脱氧胆酸对神经母细胞瘤的活性提供了支持性的临床前数据。这些发现支持在早期临床试验中进一步评估牛磺脱氧胆酸治疗复发性/难治性神经母细胞瘤患者的合理性。