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

doi:10.1016/j.ejphar.2006.12.001

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 journal › Article › peer-review

26 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 p21^Cip1/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 p21^Cip1/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 language	English
Pages (from-to)	14-20
Number of pages	7
Journal	European Journal of Pharmacology
Volume	559
Issue number	1
DOIs	https://doi.org/10.1016/j.ejphar.2006.12.001
Publication status	Published - Mar 15 2007

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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

Pharmacology

Access to Document

10.1016/j.ejphar.2006.12.001

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@article{4acc0b991a074fd29af274928a0578d2,

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

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.",

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",

author = "Hsu, \{Mei Hua\} and Chen, \{Chun Jen\} and Kuo, \{Sheng Chu\} and Chung, \{Jing Gung\} and Lai, \{Ya Yun\} and Teng, \{Che Ming\} and Pan, \{Shiow Lin\} and Huang, \{Li Jiau\}",

note = "Funding Information: The investigation was supported by research grants from the National Science Council of the Republic of China (NSC92-2323-B-039-001 and NSC95-2320-B-039-011-MY3) awarded to S.C. Kuo and L.J. Huang.",

year = "2007",

month = mar,

day = "15",

doi = "10.1016/j.ejphar.2006.12.001",

language = "English",

volume = "559",

pages = "14--20",

journal = "European Journal of Pharmacology",

issn = "0014-2999",

publisher = "Elsevier B.V.",

number = "1",

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TY - JOUR

T1 - 2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1) induces mitotic phase arrest in A549 cells

AU - Hsu, Mei Hua

AU - Chen, Chun Jen

AU - Kuo, Sheng Chu

AU - Chung, Jing Gung

AU - Lai, Ya Yun

AU - Teng, Che Ming

AU - Pan, Shiow Lin

AU - Huang, Li Jiau

N1 - Funding Information: The investigation was supported by research grants from the National Science Council of the Republic of China (NSC92-2323-B-039-001 and NSC95-2320-B-039-011-MY3) awarded to S.C. Kuo and L.J. Huang.

PY - 2007/3/15

Y1 - 2007/3/15

N2 - 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.

AB - 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.

KW - 2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1)

KW - 2-Phenyl-4-quinolone (2-PQ)

KW - A549 cells

KW - Microtubule polymerization

KW - Mitotic phase arrest

KW - p21

UR - https://www.scopus.com/pages/publications/33847187394

UR - https://www.scopus.com/pages/publications/33847187394#tab=citedBy

U2 - 10.1016/j.ejphar.2006.12.001

DO - 10.1016/j.ejphar.2006.12.001

M3 - Article

C2 - 17223102

AN - SCOPUS:33847187394

SN - 0014-2999

VL - 559

SP - 14

EP - 20

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 1

ER -

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

Abstract

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Keywords

ASJC Scopus subject areas

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