| Anti-angiogenic and anti-tumor apoptotic activities of SJ-8002, a new piperazine derivative. | |
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MedLine Citation:
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PMID: 15254733 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A new piperazine derivative, SJ-8002, is a synthetic anti-cancer agent which exhibits microtubule-inhibiting activities. In this study, we investigated the possibility that this compound inhibits angiogenesis and induces tumor-cell apoptosis using bovine aortic endothelial cells (BAECs) and human hepatocellular carcinoma cells (HepG2) as a model system, respectively. In vivo, SJ-8002 decreased the neovascularization of chick embryos and the basic fibroblast growth factor (bFGF)-induced angiogenesis in the chorioallantoic membrane (CAM) and the mouse Matrigel implants, respectively. In vitro, SJ-8002 treatment resulted in the inhibition of proliferation, migration, invasion and tube formation, and of matrix metalloproteinase-2 (MMP-2) expression in BAECs. In addition, the SJ-8002 treatment in HepG2 cells reduced cell viability, and caused the production of fragmented DNA and the morphological changes corresponding to apoptosis including condensed and fragmented DNA in a concentration-dependent manner. SJ-8002 also elicited the release of cytochrome c and the activation of caspase-3. Therefore, it is possible that SJ-8002 functions as both angiogenesis inhibitor and apoptosis inducer. Taken together, these results suggest that SJ-8002 may be a candidate for strong anti-cancer agent with the ability to inhibit the angiogenesis of endothelial cells and to induce the apoptosis of tumor cells. |
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Authors:
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Eui-Yeun Yi; Eun-Joo Jeong; Hyun Seok Song; Mi-Sook Lee; Dong-Wook Kang; Jeong-Ho Joo; Ho-Seok Kwon; Sun-Hwan Lee; Si-Kyung Park; Sun-Gan Chung; Eui-Hwan Cho; Yung-Jin Kim |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: International journal of oncology Volume: 25 ISSN: 1019-6439 ISO Abbreviation: Int. J. Oncol. Publication Date: 2004 Aug |
Date Detail:
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Created Date: 2004-07-15 Completed Date: 2005-01-25 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9306042 Medline TA: Int J Oncol Country: Greece |
Other Details:
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Languages: eng Pagination: 365-72 Citation Subset: IM |
Affiliation:
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Department of Molecular Biology, Pusan National University, Pusan 609-735, Korea. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Aminopyridines
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chemistry,
pharmacology* Angiogenesis Inhibitors / chemistry, pharmacology*, therapeutic use Animals Antineoplastic Agents / chemistry, pharmacology*, therapeutic use Apoptosis Biological Assay Caspase 3 Caspases / metabolism Cell Line, Tumor Cell Movement / drug effects Chick Embryo Collagen / drug effects Cytochromes c / metabolism Drug Combinations Laminin / drug effects Matrix Metalloproteinase 2 / drug effects Mice Neoplasms / drug therapy Neovascularization, Pathologic / drug therapy Piperazines / chemistry, pharmacology* Proteoglycans / drug effects |
| Chemical | |
Reg. No./Substance:
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0/4-(3,5-dimethylphenyl)piperazine-1-carboxylic acid (2-methoxy-5,6-dimethylpyridin-3-yl)amide; 0/Aminopyridines; 0/Angiogenesis Inhibitors; 0/Antineoplastic Agents; 0/Drug Combinations; 0/Laminin; 0/Piperazines; 0/Proteoglycans; 110-85-0/piperazine; 119978-18-6/matrigel; 9007-34-5/Collagen; 9007-43-6/Cytochromes c; EC 3.4.22.-/CASP3 protein, human; EC 3.4.22.-/Casp3 protein, mouse; EC 3.4.22.-/Caspase 3; EC 3.4.22.-/Caspases; EC 3.4.24.24/Matrix Metalloproteinase 2 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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