Dabkeviciute Girstaute, Maccioni Ellias, Petrikaite Vilma
Institute of Biotechnology, Life Sciences Center, Vilnius University Sauletekio al. 7, LT-10257, Vilnius, Lithuania.
Laboratory of Drug Targets Histopathology, Institute of Cardiology, Lithuanian University of Health Sciences Sukileliu pr. 13, LT-50162, Kaunas, Lithuania.
Am J Cancer Res. 2023 Apr 15;13(4):1377-1386. eCollection 2023.
This study aimed to evaluate the anticancer activity of 16 new sunitinib derivatives in brain cancer cells (2D model) and spheroids (3D model). The effect on cell viability was determined by the MTT assay. Single-cell migration assay was performed to examine the effect of selected compounds on individual cell migration. The activity of compounds in 3D cell cultures was examined by measuring the size change of spheroids formed using the Hanging drop method. The viability of brain cancer (U-87MG and A-172) cells was most reduced by compound EMAC4001. EMAC4001 showed the strongest effect on U-87MG cell migration, and EMAC4007 was the most active in the A-172 cell line. Only sunitinib had a statistically significant impact on spheroid growth at 100 nM and 500 nM concentrations in the U87-MG cell line and EMAC4007 had a statistically significant impact on A-172 spheroid growth at 100 nM and 500 nM concentrations, similarly to sunitinib.
本研究旨在评估16种新的舒尼替尼衍生物在脑癌细胞(二维模型)和球体(三维模型)中的抗癌活性。通过MTT法测定对细胞活力的影响。进行单细胞迁移试验以检测所选化合物对单个细胞迁移的影响。通过测量使用悬滴法形成的球体大小变化来检测化合物在三维细胞培养中的活性。化合物EMAC4001对脑癌(U-87MG和A-172)细胞活力的降低作用最为明显。EMAC4001对U-87MG细胞迁移的影响最强,而EMAC4007在A-172细胞系中活性最高。在U87-MG细胞系中,仅舒尼替尼在100 nM和500 nM浓度下对球体生长有统计学显著影响,与舒尼替尼类似,EMAC4007在100 nM和500 nM浓度下对A-172球体生长有统计学显著影响。