2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1) induces mitotic phase arrest in A549 cells

Mei Hua Hsu, Chun Jen Chen, Sheng Chu Kuo, Jing Gung Chung, Ya Yun Lai, Che Ming Teng, Shiow Lin Pan, Li Jiau Huang

Research output: Contribution to journalArticle

24 Citations (Scopus)

Abstract

A 2-phenyl-4-quinolone (2-PQ) derivative, 2-(3-fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1), was synthesized in our laboratory. In this study, we delineated the growth-inhibitory effect of YJC-1 in human lung carcinoma A549 cells. YJC-1 inhibited cell growth with an IC50 value of about 4.8 μM via microtubule polymerization, causing growth arrest in the mitotic phase. Immunoblotting analysis revealed a dramatic induction of cyclin-dependent kinase (CDK) inhibitor p21Cip1/Waf1 and down-regulation of Cdc25C phosphatase to inhibit the protein expression of cyclin B1 and CDK1. We also found that YJC-1 induced a profound time-dependent elevation in p21Cip1/Waf1 gene expression in comparison with the negative control. In vivo, we also found that YJC-1 significantly suppressed tumor growth in mice inoculated with A549 cells. These findings suggest that YJC-1 can suppress A549 cell growth via mitotic phase arrest.

Original languageEnglish
Pages (from-to)14-20
Number of pages7
JournalEuropean Journal of Pharmacology
Volume559
Issue number1
DOIs
Publication statusPublished - Mar 15 2007
Externally publishedYes

Keywords

  • 2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1)
  • 2-Phenyl-4-quinolone (2-PQ)
  • A549 cells
  • Microtubule polymerization
  • Mitotic phase arrest
  • p21

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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