Abstract
We investigated the effect of Ecklonia cava (E. cava)-derived dieckol on movement behavior and the expression of migration-related genes in MCF-7 human breast cancer cell. Phlorotannins (e.g., dieckol, 6,6'-biecko, and 2,7″-phloroglucinol-6,6'-bieckol) were purified from E. cava by using centrifugal partition chromatography. Among the phlorotannins, we found that dieckol inhibited breast cancer cell the most and was selected for further study. Radius™-well was used to assess cell migration, and dieckol (1-100 µM) was found to suppress breast cancer cell movement. Metastasis-related gene expressions were evaluated by RT-PCR and Western blot analysis. In addition, dieckol inhibited the expression of migration-related genes such as matrix metalloproteinase (MMP)-9 and vascular endothelial growth factor (VEGF). On the other hand, it stimulated the expression of tissue inhibitor of metalloproteinase (TIMP)-1 and TIMP-2. These results suggest that dieckol exerts anti-breast cancer activity via the regulation of the expressions of metastasis-related genes, and this is the first report on the anti-breast cancer effect of dieckol.
Publication types
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Comparative Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification*
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Antineoplastic Agents / pharmacology
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Benzofurans / chemistry
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Benzofurans / isolation & purification*
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Benzofurans / pharmacology
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Breast Neoplasms / drug therapy*
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Breast Neoplasms / metabolism
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Breast Neoplasms / pathology
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Cell Movement / drug effects
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Cell Survival / drug effects
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Dioxanes / chemistry
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Dioxanes / isolation & purification
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Dioxanes / pharmacology
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Dioxins / chemistry
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Dioxins / isolation & purification
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Drug Discovery*
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Female
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Gene Expression Regulation, Neoplastic / drug effects
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Humans
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MCF-7 Cells
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Matrix Metalloproteinase 9 / chemistry
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Matrix Metalloproteinase 9 / genetics
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Matrix Metalloproteinase 9 / metabolism
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Neoplasm Proteins / agonists
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Neoplasm Proteins / antagonists & inhibitors
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Neoplasm Proteins / genetics
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Neoplasm Proteins / metabolism
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Pacific Ocean
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Phaeophyceae / chemistry*
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Phaeophyceae / growth & development
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Phloroglucinol / analogs & derivatives
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Phloroglucinol / chemistry
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Phloroglucinol / isolation & purification
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Phloroglucinol / pharmacology
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Republic of Korea
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Seaweed / chemistry*
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Seaweed / growth & development
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Tannins / chemistry
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Tannins / isolation & purification*
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Tannins / pharmacology
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Tissue Inhibitor of Metalloproteinase-1 / agonists
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Tissue Inhibitor of Metalloproteinase-1 / genetics
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Tissue Inhibitor of Metalloproteinase-1 / metabolism
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Tissue Inhibitor of Metalloproteinase-2 / agonists
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Tissue Inhibitor of Metalloproteinase-2 / genetics
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Tissue Inhibitor of Metalloproteinase-2 / metabolism
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Vascular Endothelial Growth Factor A / antagonists & inhibitors
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Vascular Endothelial Growth Factor A / genetics
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Vascular Endothelial Growth Factor A / metabolism
Substances
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2,7''-phloroglucinol-6,6'-bieckol
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Antineoplastic Agents
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Benzofurans
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Dioxanes
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Dioxins
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Neoplasm Proteins
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TIMP1 protein, human
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TIMP2 protein, human
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Tannins
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Tissue Inhibitor of Metalloproteinase-1
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VEGFA protein, human
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Vascular Endothelial Growth Factor A
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dieckol
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Tissue Inhibitor of Metalloproteinase-2
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6,6'-bieckol
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Phloroglucinol
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MMP9 protein, human
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Matrix Metalloproteinase 9