A Benzochalcone Derivative, (E)‎-1-(2-hydroxy-6-methoxyphenyl)‎-3-(naphthalen-2-yl)‎prop-2-en-1-one (DK-512)‎, Inhibits Tumor Invasion through Inhibition of the TNFα-Induced NF-κBMMP-9 Axis in MDA-MB-231 Breast Cancer Cells

Abstract EN

Tumor invasion is a critical step in tumor metastasis.

In this study, we synthesized a novel benzochalcone derivative, (E)-1-(2-hydroxy-6-methoxyphenyl)-3-(naphthalen-2-yl) prop-2-en-1-one (DK-512), and characterized its effects on tumor invasion and its mechanism of action.

We found that DK-512 strongly inhibited invasion of metastatic MDA-MB-231 breast cancer cells as revealed by a three-dimensional spheroid culture system.

Tumor invasion and metastasis require disruption of the extracellular matrix.

Matrix metalloproteinase-9 (MMP-9) is an endopeptidase that degrades extracellular matrix components.

DK-512 significantly reduced tumor necrosis factor-α- (TNFα-) induced MMP-9 mRNA expression through the inhibition of RelA nuclear factor- (NF-) κB transcription factor.

As our study was assessed in vitro, further works about in vivo efficacy of DK-512 are needed to gain further insights into whether DK-512 could be utilized as a scaffold for the development of antimetastatic agents for breast cancer.