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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells
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 str...
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2016-01-01
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Series: | Journal of Chemistry |
Online Access: | http://dx.doi.org/10.1155/2016/4921717 |
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author | Soon Young Shin Chang Gun Kim Seunghyun Ahn You Jung Jung Dongsoo Koh Young Han Lee Yoongho Lim |
author_facet | Soon Young Shin Chang Gun Kim Seunghyun Ahn You Jung Jung Dongsoo Koh Young Han Lee Yoongho Lim |
author_sort | Soon Young Shin |
collection | DOAJ |
description | 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. |
format | Article |
id | doaj-art-6c4d61f90ccd4a23a6fe59ee28f00137 |
institution | Kabale University |
issn | 2090-9063 2090-9071 |
language | English |
publishDate | 2016-01-01 |
publisher | Wiley |
record_format | Article |
series | Journal of Chemistry |
spelling | doaj-art-6c4d61f90ccd4a23a6fe59ee28f001372025-02-03T05:43:53ZengWileyJournal of Chemistry2090-90632090-90712016-01-01201610.1155/2016/49217174921717A 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer CellsSoon Young Shin0Chang Gun Kim1Seunghyun Ahn2You Jung Jung3Dongsoo Koh4Young Han Lee5Yoongho Lim6Department of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, Seoul 05029, Republic of KoreaCancer and Metabolism Institute, Konkuk University, Seoul 05029, Republic of KoreaDivision of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 05029, Republic of KoreaCancer and Metabolism Institute, Konkuk University, Seoul 05029, Republic of KoreaDepartment of Applied Chemistry, Dongduk Women’s University, Seoul 02748, Republic of KoreaDepartment of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, Seoul 05029, Republic of KoreaDivision of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 05029, Republic of KoreaTumor 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.http://dx.doi.org/10.1155/2016/4921717 |
spellingShingle | Soon Young Shin Chang Gun Kim Seunghyun Ahn You Jung Jung Dongsoo Koh Young Han Lee Yoongho Lim 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells Journal of Chemistry |
title | 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells |
title_full | 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells |
title_fullStr | 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells |
title_full_unstemmed | 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells |
title_short | 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-κB/MMP-9 Axis in MDA-MB-231 Breast Cancer Cells |
title_sort | 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 κb mmp 9 axis in mda mb 231 breast cancer cells |
url | http://dx.doi.org/10.1155/2016/4921717 |
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