Document Detail


Novel quinolone CHM-1 induces apoptosis and inhibits metastasis in a human osterogenic sarcoma cell line.
MedLine Citation:
PMID:  19557855     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Novel 2-phenyl-4-quinolone compounds have potent cytotoxic effects on different human cancer cell lines. In this study, we examined anticancer activity and mechanisms of 20-fluoro-6,7-methylenedioxy-2-phenyl-4-quinolone (CHM-1) in human osterogenic sarcoma U-2 OS cells. CHM-1-induced apoptosis was determined by flow cytometric analysis, DAPI staining, Comet assay, and caspase inhibitors. CHM-1-inhibited cell migration and invasion was assessed by a wound healing assay, gelatin zymography, and a Transwell assay. The mechanisms of CHM-1 effects on apoptosis and metastasis signaling pathways were studied using Western blotting and gene expression. CHM-1 induced G2/M arrest and apoptosis at an IC(50) (3 microM) in U-2 OS cells and caspase-3, -8, and -9 were activated. Caspase inhibitors increased cell viability after exposure to CHM-1. CHM-1-induced apoptosis was associated with enhanced ROS generation, DNA damage, decreased DeltaPsi(m) levels, and promotion of mitochondrial cytochrome c release. CHM-1 stimulated mRNA expression of caspase-3, -8, and -9, AIF, and Endo G. In addition, CHM-1 inhibited cell metastasis at a low concentration (<3 microM). CHM-1 inhibited the cell metastasis through the inhibition of MMP-2, -7, and -9. CHM-1 also decreased the levels of MAPK signaling pathways before leading to the inhibition of MMPs. In summary, CHM-1 is a potent inducer of apoptosis, which plays a role in the anticancer activity of CHM-1.
Authors:
Shu-Chun Hsu; Jai-Sing Yang; Chao-Lin Kuo; Chyi Lo; Jing-Pin Lin; Te-Chun Hsia; Jen-Jyh Lin; Kuang-Chi Lai; Hsiu-Maan Kuo; Li-Jiau Huang; Sheng-Chu Kuo; W Gibson Wood; Jing-Gung Chung
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of orthopaedic research : official publication of the Orthopaedic Research Society     Volume:  27     ISSN:  1554-527X     ISO Abbreviation:  J. Orthop. Res.     Publication Date:  2009 Dec 
Date Detail:
Created Date:  2009-12-28     Completed Date:  2010-09-02     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8404726     Medline TA:  J Orthop Res     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1637-44     Citation Subset:  IM    
Affiliation:
School of Nutrition, China Medical University, Taichung, Taiwan.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents / pharmacology*
Bone Neoplasms / drug therapy*,  genetics,  pathology
Caspases / antagonists & inhibitors,  biosynthesis
Cell Line, Tumor
Cell Movement / drug effects
Cell Survival / drug effects
Comet Assay
DNA Damage
Dioxoles / pharmacology*
Drug Screening Assays, Antitumor
Enzyme Inhibitors / pharmacology
Gene Expression / drug effects
Humans
MAP Kinase Signaling System / drug effects
Matrix Metalloproteinase 9 / antagonists & inhibitors*
Mitogen-Activated Protein Kinases / metabolism
Osteosarcoma / drug therapy*,  genetics,  pathology
Quinolones / pharmacology*
Reactive Oxygen Species / metabolism
Chemical
Reg. No./Substance:
0/2'-fluoro-6,7-methylenedioxy-2-phenyl-4-quinolone; 0/Antineoplastic Agents; 0/Dioxoles; 0/Enzyme Inhibitors; 0/Quinolones; 0/Reactive Oxygen Species; EC 2.7.11.24/Mitogen-Activated Protein Kinases; EC 3.4.22.-/Caspases; EC 3.4.24.35/Matrix Metalloproteinase 9

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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