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

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Title:	2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1) induces mitotic phase arrest in A549 cells.
Authors:	(Mei-Hua Hsu);(Chun-Jen Chen);郭盛助(Sheng-Chu Kuo);鍾景光(Jing-Gung Chung);(Ya-Yun Lai);(Che-Ming Teng);(Shiow-Lin Pan);黃麗嬌(Li-Jiau Huang)*
Contributors:	藥學院藥物化學研究所
Keywords:	2-Phenyl-4-quinolone (2-PQ);2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1);Mitotic phase arrest;Microtubule polymerization;p21Cip1/Waf1;A549 cells
Date:	2007-03
Issue Date:	2009-08-26 16:27:00 (UTC+8)
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.
Relation:	EUROPEAN JOURNAL OF PHARMACOLOGY 559(1 )14 ~20
Appears in Collections:	[Graduate Institute of Pharmaceutical Chemistry] Journal articles

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