Anti-cancer effects of 2-oxoquinoline derivatives on the HCT116 and LoVo human colon cancer cell lines

  • Authors:
    • Feng-Qi Fang
    • Hui-Shu Guo
    • Jie Zhang
    • Li-Ying Ban
    • Ji-Wei Liu
    • Pei-Yao Yu
  • View Affiliations

  • Published online on: October 16, 2015     https://doi.org/10.3892/mmr.2015.4451
  • Pages: 8062-8070
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Abstract

The present study demonstrated the anti-tumor effects of the quinoline derivative [5-(3-chloro-oxo-4-phenyl-cyclobutyl)-quinoli-8-yl-oxy] acetic acid hydrazide (CQAH) against colorectal carcinoma. Substantial apoptotic effects of CQAH on HCT116 and LoVo human colon cancer cell lines were observed. Apoptosis was identified based on cell morphological characteristics, including cell shrinkage and chromatin condensation as well as Annexin V/propidium iodide double staining followed by flow cytometric analysis and detection of apoptosis-associated proteins by western blot analysis. CQAH induced caspase-3 and PARP cleavage, reduced the expression of the anti-apoptotic proteins myeloid cell leukemia-1 and B-cell lymphoma (Bcl) extra large protein and elevated the expression of the pro-apoptotic protein Bcl-2 homologous antagonist killer. In addition, pharmacological inhibition of c-Jun N-terminal kinase (JNK), but not extracellular signal-regulated kinase or p38, significantly reduced CQAH-mediated cell death as well as cleavage of caspase-3 and PARP. Co-treatment of CQAH with the commercial chemotherapeutics 5-fluorouracil and camptothecin-11 significantly improved their efficacies. Comparison of the apoptotic effects of CQAH with those of two illustrated structure-activity associations for this compound type, indicating that substitution at position-4 of the azetidine phenyl ring is pivotal for inducing apoptosis. In conclusion, the results of the present study indicated CQAH and its analogues are potent candidate drugs for the treatment of colon carcinoma.
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December-2015
Volume 12 Issue 6

Print ISSN: 1791-2997
Online ISSN:1791-3004

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Spandidos Publications style
Fang F, Guo H, Zhang J, Ban L, Liu J and Yu P: Anti-cancer effects of 2-oxoquinoline derivatives on the HCT116 and LoVo human colon cancer cell lines. Mol Med Rep 12: 8062-8070, 2015
APA
Fang, F., Guo, H., Zhang, J., Ban, L., Liu, J., & Yu, P. (2015). Anti-cancer effects of 2-oxoquinoline derivatives on the HCT116 and LoVo human colon cancer cell lines. Molecular Medicine Reports, 12, 8062-8070. https://doi.org/10.3892/mmr.2015.4451
MLA
Fang, F., Guo, H., Zhang, J., Ban, L., Liu, J., Yu, P."Anti-cancer effects of 2-oxoquinoline derivatives on the HCT116 and LoVo human colon cancer cell lines". Molecular Medicine Reports 12.6 (2015): 8062-8070.
Chicago
Fang, F., Guo, H., Zhang, J., Ban, L., Liu, J., Yu, P."Anti-cancer effects of 2-oxoquinoline derivatives on the HCT116 and LoVo human colon cancer cell lines". Molecular Medicine Reports 12, no. 6 (2015): 8062-8070. https://doi.org/10.3892/mmr.2015.4451