-
Anti-cancer Effects of a Novel Quinoline Derivative 83b1 on Human Esophageal Squamous Cell Carcinoma through Down-Regulation of COX-2 mRNA and PGE2
-
Ivan Ho Yuen Pun, Dessy Chan, Sau Hing Chan, Po Yee Chung, Yuan Yuan Zhou, Simon Law, Alfred King Yin Lam, Chung Hin Chui, Albert Sun Chi Chan, Kim Hung Lam, Johnny Cheuk On Tang
-
Cancer Res Treat. 2017;49(1):219-229. Published online July 18, 2016
-
DOI: https://doi.org/10.4143/crt.2016.190
-
-
Abstract
PDFSupplementary MaterialPubReaderePub
- Purpose
83b1 is a novel quinoline derivative that has been shown to inhibit cancer growth in human esophageal squamous cell carcinoma (ESCC). This study was conducted to comprehensively evaluate the cytotoxic effects of 83b1 on a series of ESCC cell lines and investigate the mechanisms by which 83b1 suppresses cancer growth based on molecular docking analysis.
Materials and Methods
A series of ESCC and nontumor immortalized cell lines were exposed to 83b1 and cisplatin (CDDP) in a dose-dependent manner, and the cytotoxicity was examined by a MTS assay kit. Prediction of the molecular targets of 83b1 was conducted by molecular docking analysis. Expression of cyclooxygenase 2 (COX-2) mRNA and COX-2–derived prostaglandin E2 (PGE2) were measured by quantitative real-time polymerase chain reaction and enzymelinked immuno-sorbent assay, respectively. In vivo anti-tumor effect was determined using a nude mice xenografted model transplanted with an ESCC cell line, KYSE-450.
Results
83b1 showed the significant anti-cancer effects on all ESCC cell lines compared to CDDP; however, 83b1 revealed much lower toxic effects on non-tumor cell lines than CDDP. The predicted molecular target of 83b1 is peroxisome proliferator-activated receptor delta (PPARδ), which is a widely known oncoprotein. Additionally the expression of COX-2 mRNA and COX-2–derived PGE2 were down-regulated by 83b1 in a dose-dependent manner in ESCC cell lines. Furthermore, 83b1 was shown to significantly reduce the tumor size in nude mice xenograft.
Conclusion
The results of this study suggest that the potential anti-cancer effects of 83b1 on human esophageal cancers occur through the possible oncotarget, PPARδ, and down-regulation of the cancer related genes and molecules.
-
Citations
Citations to this article as recorded by
- Synthesis and biological evaluation of novel 2-morpholino-4-anilinoquinoline derivatives as antitumor agents against HepG2 cell line
Ahmed Al-Sheikh, Malak A. Jaber, Hana'a Khalaf, Nour AlKhawaja, Duaa Abuarqoub RSC Advances.2024; 14(5): 3304. CrossRef - Natural alkaloids as potential treatments for esophageal squamous-cell carcinoma: A comprehensive review
Eugene Jamot Ndebia, Gabriel Tchuente Kamsu Gastroenterology & Endoscopy.2024; 2(3): 131. CrossRef - Arachidonic acid metabolism as a novel pathogenic factor in gastrointestinal cancers
Weiqin Lu, Aihemaitijiang Aihaiti, Paziliya Abudukeranmu, Yajun Liu, Huihui Gao Molecular and Cellular Biochemistry.2024;[Epub] CrossRef - Downregulation of chemokine (C‑C motif) ligand 5 induced by a novel 8‑hydroxyquinoline derivative (91b1) suppresses tumor invasiveness in esophageal carcinoma
Johnny Tang, Dessy Chan, Po-Yee Chung, Yijiang Liu, Alfred Lam, Simon Law, Wolin Huang, Albert Chan, Kim-Hung Lam, Yuanyuan Zhou International Journal of Molecular Medicine.2024;[Epub] CrossRef - Peroxisome proliferator-activated receptors regulate the progression and treatment of gastrointestinal cancers
Min Zhang, Shujie He Frontiers in Pharmacology.2023;[Epub] CrossRef - Roles of Nuclear Receptors in Esophageal Cancer
Lihao Deng, Jiaxuan Liu, Wei-Dong Chen, Yan-Dong Wang Current Pharmaceutical Biotechnology.2023; 24(12): 1489. CrossRef - Synthesis and biological activities of new phthalimide and thiazolidine derivatives
Flaviana A. Santos, Marcel L. Almeida, Vitor A. S. Silva, Douglas C. F. Viana, Michelly C. Pereira, André S. L. Lucena, Maira G. R. Pitta, Marina R. Galdino-Pitta, Moacyr J. B. de Melo Rêgo, Ivan da Rocha Pitta Medicinal Chemistry Research.2022; 31(1): 108. CrossRef - Role of Prostaglandin E2 in the Progression of Gastrointestinal Cancer
David Jay Wilson, Raymond N. DuBois Cancer Prevention Research.2022; 15(6): 355. CrossRef - The Anticancer Effect of a Novel Quinoline Derivative 91b1 through Downregulation of Lumican
Yuanyuan Zhou, Zhongguo Zhou, Dessy Chan, Po yee Chung, Yongqi Wang, Albert Sun chi Chan, Simon Law, Kim hung Lam, Johnny Cheuk On Tang International Journal of Molecular Sciences.2022; 23(21): 13181. CrossRef - Synthesis and biological evaluations of N′-substituted methylene-4-(quinoline-4-amino) benzoylhydrazides as potential anti-hepatoma agents
Baicun Li, Feifeng Zhu, Fengming He, Qingqing Huang, Xiaoguang Liu, Tong Wu, Taige Zhao, Yingkun Qiu, Zhen Wu, Yuhua Xue, Meijuan Fang Bioorganic Chemistry.2020; 96: 103592. CrossRef - Feasibility of Repurposing Clioquinol for Cancer Therapy
Raheel Khan, Harras Khan, Yassen Abdullah, Q. Ping Dou Recent Patents on Anti-Cancer Drug Discovery.2020; 15(1): 14. CrossRef - DFIQ, a Novel Quinoline Derivative, Shows Anticancer Potential by Inducing Apoptosis and Autophagy in NSCLC Cell and In Vivo Zebrafish Xenograft Models
Hurng-Wern Huang, Yung-Ding Bow, Chia-Yih Wang, Yen-Chun Chen, Pei-Rong Fu, Kuo-Feng Chang, Tso-Wen Wang, Chih-Hua Tseng, Yeh-Long Chen, Chien-Chih Chiu Cancers.2020; 12(5): 1348. CrossRef - Reverse Screening Methods to Search for the Protein Targets of Chemopreventive Compounds
Hongbin Huang, Guigui Zhang, Yuquan Zhou, Chenru Lin, Suling Chen, Yutong Lin, Shangkang Mai, Zunnan Huang Frontiers in Chemistry.2018;[Epub] CrossRef - The roles of the COX2/PGE2/EP axis in therapeutic resistance
Dali Tong, Qiuli Liu, Lin-ang Wang, Qiubo Xie, Jian Pang, Yiqiang Huang, Luofu Wang, Gaolei Liu, Dianzheng Zhang, Weihua Lan, Jun Jiang Cancer and Metastasis Reviews.2018; 37(2-3): 355. CrossRef - Expression of Insulin-Like Growth Factor Binding Protein-5 (IGFBP5) Reverses Cisplatin-Resistance in Esophageal Carcinoma
Dessy Chan, Yuanyuan Zhou, Chung Hin Chui, Kim Hung Lam, Simon Law, Albert Sun-chi Chan, Xingshu Li, Alfred King-yin Lam, Johnny Cheuk On Tang Cells.2018; 7(10): 143. CrossRef - Targeting DNA Binding for NF-κB as an Anticancer Approach in Hepatocellular Carcinoma
Po Chung, Pik Lam, Yuanyuan Zhou, Jessica Gasparello, Alessia Finotti, Adriana Chilin, Giovanni Marzaro, Roberto Gambari, Zhaoxiang Bian, Wai Kwok, Wai Wong, Xi Wang, Alfred Lam, Albert Chan, Xingshu Li, Jessica Ma, Chung Chui, Kim Lam, Johnny Tang Cells.2018; 7(10): 177. CrossRef
-
10,881
View
-
254
Download
-
20
Web of Science
-
16
Crossref
|