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Novel eIF4E/eIF4G protein-protein interaction inhibitors DDH-1 exhibits anti-cancer activity in vivo and in vitro
Wang, Jun1; Wang, Lijun2; Zhang, Shuhong3; Fan, Junting4; Yang, Hui1; Li, Qiqi1; Guo, Chuanlong1
2020-10-01
Source PublicationINTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
ISSN0141-8130
Volume160Pages:496-505
Corresponding AuthorGuo, Chuanlong(guochuanlong@qust.edu.cn)
Abstract(E)-2-(2-(2,3-dibromo-4,5-dimethoxybenzylidene)hydrazinyl)-4-(3,4-difluorophenyl) thiazole (DDH-1) is novel small molecule compound synthesized in our previous work. This study found that DDH-1 could inhibit the proliferation of various human lung cancer cells. Particularly, the IC50 for A549 cells was 8.59 AM. Interestingly, we found that DDH-1 inhibits eIF4E/eIF4G interaction. The flow cytometry (FAGS) results have indicated that DDH-1 may induce G0/G1 cycle arrest by inhibiting the expression of Cyclin D1 and CDK4. DDH-1 may also cause apoptosis through the caspase-dependent pathway. Study of these mechanisms has shown that DDH-1 may prompt reactive oxygen species (ROS) generation, decrease the mitochondrial membrane potential (MMP), and stimulate DNA double-strand breaks (DSBs) in A549 cells. Study of the signal pathway has indicated that DDH-1 could activate JNK phosphorylation and inhibit ERK phosphorylation. Interestingly, NAC, which scavenges ROS, reversed the MMP decline, DNA damage, JNK phosphorylation activation, and ERK phosphorylation inhibition caused by DDH-1. Overall, these findings provide evidence that the eIF4E/eIF4G interaction inhibitors DDH-1 induces DNA damage and apoptosis in human lung cancer A549 cells. (C) 2020 Elsevier B.V. All rights reserved.
KeywordeIF4E/eIF4G Human lung cancer Apoptosis DNA damage ROS
DOI10.1016/j.ijbiomac.2020.05.233
Indexed BySCI
Language英语
Funding ProjectNational Natural Science Foundation of China[81773586]
WOS Research AreaBiochemistry & Molecular Biology ; Chemistry ; Polymer Science
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Applied ; Polymer Science
WOS IDWOS:000564748800017
PublisherELSEVIER
Citation statistics
Cited Times:1[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.qdio.ac.cn/handle/337002/168508
Collection实验海洋生物学重点实验室
Corresponding AuthorGuo, Chuanlong
Affiliation1.Qingdao Univ Sci & Technol, Coll Chem Engn, Dept Pharm, Qingdao 266042, Peoples R China
2.Chinese Acad Sci, Inst Oceanol, CAS Key Lab Expt Marine Biol, Qingdao 266071, Peoples R China
3.Qingdao Chengyang Peoples Hosp, Qingdao 266109, Peoples R China
4.Nanjing Med Univ, Sch Pharm, Dept Pharmaceut Anal, Nanjing 211166, Peoples R China
Recommended Citation
GB/T 7714
Wang, Jun,Wang, Lijun,Zhang, Shuhong,et al. Novel eIF4E/eIF4G protein-protein interaction inhibitors DDH-1 exhibits anti-cancer activity in vivo and in vitro[J]. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,2020,160:496-505.
APA Wang, Jun.,Wang, Lijun.,Zhang, Shuhong.,Fan, Junting.,Yang, Hui.,...&Guo, Chuanlong.(2020).Novel eIF4E/eIF4G protein-protein interaction inhibitors DDH-1 exhibits anti-cancer activity in vivo and in vitro.INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,160,496-505.
MLA Wang, Jun,et al."Novel eIF4E/eIF4G protein-protein interaction inhibitors DDH-1 exhibits anti-cancer activity in vivo and in vitro".INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES 160(2020):496-505.
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