Department of Medicine, Clinic III-Hematology, Oncology, Palliative Medicine, University of Rostock, 18057 Rostock, Germany.
Small Animal Clinic, University of Veterinary Medicine Hannover, 30559 Hannover, Germany.
Int J Mol Sci. 2019 Nov 7;20(22):5567. doi: 10.3390/ijms20225567.
Current therapies are insufficient for metastatic prostate cancer (PCa) in men and dogs. As human castrate-resistant PCa shares several characteristics with the canine disease, comparative evaluation of novel therapeutic agents is of considerable value for both species. Novel isoquinolinamine FX-9 exhibits antiproliferative activity in acute lymphoblastic leukemia cell lines but has not been tested yet on any solid neoplasia type. In this study, FX-9's mediated effects were characterized on two human (PC-3, LNCaP) and two canine (CT1258, 0846) PCa cell lines, as well as benign solid tissue cells. FX-9 significantly inhibited cell viability and induced apoptosis with concentrations in the low micromolar range. Mediated effects were highly comparable between the PCa cell lines of both species, but less pronounced on non-malignant chondrocytes and fibroblasts. Interestingly, FX-9 exposure also leads to the formation and survival of enlarged multinucleated cells through mitotic slippage. Based on the results, FX-9 acts as an anti-mitotic agent with reduced cytotoxic activity in benign cells. The characterization of FX-9-induced effects on PCa cells provides a basis for in vivo studies with the potential of valuable transferable findings to the benefit of men and dogs.
目前的治疗方法对于男性和犬类的转移性前列腺癌 (PCa) 都不够有效。由于人类去势抵抗性 PCa 与犬类疾病有几个共同特点,因此对新型治疗药物进行比较评估对这两个物种都具有相当大的价值。新型异喹啉胺 FX-9 在急性淋巴细胞白血病细胞系中具有抗增殖活性,但尚未在任何实体肿瘤类型上进行测试。在这项研究中,研究人员对两种人源 (PC-3、LNCaP) 和两种犬源 (CT1258、0846) PCa 细胞系以及良性实体组织细胞进行了 FX-9 介导的作用特征分析。FX-9 在低微摩尔浓度范围内显著抑制细胞活力并诱导细胞凋亡。在这两个物种的 PCa 细胞系之间,介导的作用非常相似,但对非恶性软骨细胞和成纤维细胞的作用不太明显。有趣的是,FX-9 暴露还会导致多核细胞的形成和存活,这是通过有丝分裂滑走实现的。基于这些结果,FX-9 作为一种抗有丝分裂药物,在良性细胞中具有降低的细胞毒性活性。FX-9 诱导的 PCa 细胞作用的特征为体内研究提供了基础,具有将有价值的可转移发现应用于人类和犬类的潜力。