Li J, Wang A, Li N, Zhu Y, Li K, Liu H, Gao Z
Department of Ophthalmology, First Affiliated Hospital of Bengbu Medical College, Bengbu 233000, China.
Institute of Biomedical and Health Science, School of Life and Health Science, Anhui Science and Technology University, Fengyang 233100, China.
Nan Fang Yi Ke Da Xue Xue Bao. 2022 Nov 20;42(11):1604-1610. doi: 10.12122/j.issn.1673-4254.2022.11.03.
To investigate the inhibitory effect of aumolertinib on proliferation of human choroidal melanoma MUM-2B cells and explore the possible molecular mechanism.
CCK-8 assay and colony formation assay were used to evaluate the inhibitory effect of different concentrations of aumolertinib on viability and proliferation of MUM-2B cells. Flow cytometry was performed to analyze the apoptosis, necrosis, cellular ROS production and cell cycle changes in aumolertinib- treated MUM-2B cells. The antitumor effect of aumolertinib against human choroidal melanoma was observed in nude mouse models bearing MUM-2B tumor cell xenografts.
The results of CCK-8 and colony formation assay showed that aumolertinib strongly inhibited the proliferation MUM-2B cells in a dose-dependent manner. Flow cytometry showed that aumolertinib dose-dependently increased the total apoptosis rate of MUM-2B cells to as high as 76.65% at the concentration of 8 μmol/L and induced obvious cell cycle arrest at G1 phase. Aumolertinib treatment also caused a dose-dependent increase of ROS production and reduction of mitochondrial membrane potential in MUM-2B cells. In the tumor-bearing nude mice, treatment with aumolertinib significantly inhibited tumor growth without causing obvious body weight loss.
Aumolertinib can effectively inhibit the growth of human choroidal melanoma MUM-2B cells both and , suggesting its potential clinical value in the therapy of choroidal melanomas.
研究奥莫替尼对人脉络膜黑色素瘤MUM-2B细胞增殖的抑制作用,并探讨其可能的分子机制。
采用CCK-8法和集落形成试验评估不同浓度奥莫替尼对MUM-2B细胞活力和增殖的抑制作用。运用流式细胞术分析经奥莫替尼处理的MUM-2B细胞的凋亡、坏死、细胞活性氧生成及细胞周期变化。在荷MUM-2B肿瘤细胞异种移植瘤的裸鼠模型中观察奥莫替尼对人脉络膜黑色素瘤的抗肿瘤作用。
CCK-8法和集落形成试验结果显示,奥莫替尼以剂量依赖性方式强烈抑制MUM-2B细胞增殖。流式细胞术表明,奥莫替尼在8 μmol/L浓度时剂量依赖性地将MUM-2B细胞的总凋亡率提高至76.65%,并诱导明显的G1期细胞周期阻滞。奥莫替尼处理还导致MUM-2B细胞中活性氧生成呈剂量依赖性增加以及线粒体膜电位降低。在荷瘤裸鼠中,奥莫替尼治疗显著抑制肿瘤生长,且未引起明显体重减轻。
奥莫替尼在体外和体内均可有效抑制人脉络膜黑色素瘤MUM-2B细胞的生长,提示其在脉络膜黑色素瘤治疗中具有潜在的临床价值。