Aumolertinib inhibits growth of human choroidal melanoma MUM-2B cells in vitro and in vivo.
10.12122/j.issn.1673-4254.2022.11.03
- Author:
Juan LI
1
;
Ai Lian WANG
1
;
Ning LI
1
;
Ying Ze ZHU
2
;
Kun LI
2
;
Hao LIU
3
;
Zi Qing GAO
1
Author Information
1. Department of Ophthalmology, First Affiliated Hospital of Bengbu Medical College, Bengbu 233000, China.
2. Institute of Biomedical and Health Science, School of Life and Health Science, Anhui Science and Technology University, Fengyang 233100, China.
3. School of Pharmacy, Bengbu Medical College, Bengbu 233030, China.
- Publication Type:Journal Article
- Keywords:
aumolertinib;
epidermal growth factor receptor;
human choroidal melanoma
- MeSH:
Animals;
Mice;
Humans;
Mice, Nude;
Sincalide;
Indoles;
Melanoma/drug therapy*
- From:
Journal of Southern Medical University
2022;42(11):1604-1610
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To investigate the inhibitory effect of aumolertinib on proliferation of human choroidal melanoma MUM-2B cells and explore the possible molecular mechanism.
METHODS: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.
RESULTS: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.
CONCLUSION:Aumolertinib can effectively inhibit the growth of human choroidal melanoma MUM-2B cells both in vivo and in vitro, suggesting its potential clinical value in the therapy of choroidal melanomas.