First evidence that Ecklonia cava-derived dieckol attenuates MCF-7 human breast carcinoma cell migration

Mar Drugs. 2015 Mar 30;13(4):1785-97. doi: 10.3390/md13041785.

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

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / isolation & purification*
  • Antineoplastic Agents / pharmacology
  • Benzofurans / chemistry
  • Benzofurans / isolation & purification*
  • Benzofurans / pharmacology
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Movement / drug effects
  • Cell Survival / drug effects
  • Dioxanes / chemistry
  • Dioxanes / isolation & purification
  • Dioxanes / pharmacology
  • Dioxins / chemistry
  • Dioxins / isolation & purification
  • Drug Discovery*
  • Female
  • Gene Expression Regulation, Neoplastic / drug effects
  • Humans
  • MCF-7 Cells
  • Matrix Metalloproteinase 9 / chemistry
  • Matrix Metalloproteinase 9 / genetics
  • Matrix Metalloproteinase 9 / metabolism
  • Neoplasm Proteins / agonists
  • Neoplasm Proteins / antagonists & inhibitors
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / metabolism
  • Pacific Ocean
  • Phaeophyceae / chemistry*
  • Phaeophyceae / growth & development
  • Phloroglucinol / analogs & derivatives
  • Phloroglucinol / chemistry
  • Phloroglucinol / isolation & purification
  • Phloroglucinol / pharmacology
  • Republic of Korea
  • Seaweed / chemistry*
  • Seaweed / growth & development
  • Tannins / chemistry
  • Tannins / isolation & purification*
  • Tannins / pharmacology
  • Tissue Inhibitor of Metalloproteinase-1 / agonists
  • Tissue Inhibitor of Metalloproteinase-1 / genetics
  • Tissue Inhibitor of Metalloproteinase-1 / metabolism
  • Tissue Inhibitor of Metalloproteinase-2 / agonists
  • Tissue Inhibitor of Metalloproteinase-2 / genetics
  • Tissue Inhibitor of Metalloproteinase-2 / metabolism
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vascular Endothelial Growth Factor A / genetics
  • Vascular Endothelial Growth Factor A / metabolism

Substances

  • 2,7''-phloroglucinol-6,6'-bieckol
  • Antineoplastic Agents
  • Benzofurans
  • Dioxanes
  • Dioxins
  • Neoplasm Proteins
  • TIMP1 protein, human
  • TIMP2 protein, human
  • Tannins
  • Tissue Inhibitor of Metalloproteinase-1
  • VEGFA protein, human
  • Vascular Endothelial Growth Factor A
  • dieckol
  • Tissue Inhibitor of Metalloproteinase-2
  • 6,6'-bieckol
  • Phloroglucinol
  • MMP9 protein, human
  • Matrix Metalloproteinase 9