https://scholars.lib.ntu.edu.tw/handle/123456789/328306
標題: | 2-(3-Fluorophenyl)-6-methoxyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (YJC-1) induces mitotic phase arrest in A549 cells | 作者: | CHE-MING TENG | 關鍵字: | 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; p21Cip1/Waf1 | 公開日期: | 2007 | 卷: | 559 | 期: | 1 | 起(迄)頁: | 14-20 | 來源出版物: | European Journal of Pharmacology | 摘要: | 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. ? 2007. |
URI: | http://www.scopus.com/inward/record.url?eid=2-s2.0-33847187394&partnerID=MN8TOARS http://scholars.lib.ntu.edu.tw/handle/123456789/328306 |
DOI: | 10.1016/j.ejphar.2006.12.001 | SDG/關鍵字: | 2 (3 fluorophenyl) 6 methoxyl 4 oxo 1,4 dihydroquinoline 3 carboxylic acid; cyclin dependent kinase inhibitor 1; cyclin dependent kinase inhibitor 1A; quinolone derivative; unclassified drug; yjc 1; article; cancer inhibition; cell cycle arrest; controlled study; cytotoxicity; drug structure; gene expression; human; human cell; IC 50; immunoblotting; lung carcinoma; microtubule assembly; mitosis; priority journal; Antimitotic Agents; Blotting, Western; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Survival; Cyclin-Dependent Kinase Inhibitor p21; Flow Cytometry; G0 Phase; Humans; Microscopy, Fluorescence; Microtubules; Mitosis; Reverse Transcriptase Polymerase Chain Reaction; Xenograft Model Antitumor Assays |
顯示於: | 醫學系 |
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