Kim Eun-Kyung, Tang Yujiao, Kim Yon-Suk, Hwang Jin-Woo, Choi Eun-Ju, Lee Ji-Hyeok, Lee Seung-Hong, Jeon You-Jin, Park Pyo-Jam
Division of Food Bio Science, College of Biomedical and Health Sciences, Konkuk University, Chungju 380-701, Korea.
Korea Nokyong Research Center, Konkuk University, Chungju 380-701, Korea.
Mar Drugs. 2015 Mar 30;13(4):1785-97. doi: 10.3390/md13041785.
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.
我们研究了海带（Ecklonia cava，E. cava）衍生的二eckol对MCF-7人乳腺癌细胞运动行为及迁移相关基因表达的影响。通过离心分配色谱法从海带中纯化出了间苯三酚单宁（如二eckol、6,6'-联eckol和2,7″-间苯三酚-6,6'-联eckol）。在这些间苯三酚单宁中，我们发现二eckol对乳腺癌细胞的抑制作用最强，并选择其进行进一步研究。使用Radius™孔板评估细胞迁移，发现二eckol（1-100μM）可抑制乳腺癌细胞的运动。通过逆转录聚合酶链反应（RT-PCR）和蛋白质免疫印迹分析评估转移相关基因的表达。此外，二eckol抑制了基质金属蛋白酶（MMP）-9和血管内皮生长因子（VEGF）等迁移相关基因的表达。另一方面，它刺激了金属蛋白酶组织抑制剂（TIMP）-1和TIMP-2的表达。这些结果表明，二eckol通过调节转移相关基因的表达发挥抗乳腺癌活性，这是关于二eckol抗乳腺癌作用的首次报道。
