Targeting of MMP-9 could be a useful approach for anticancer therapy. The inhibitory activities
of 23 flavonoids on tumor necrosis factors alpha (TNF)-induced matrix metalloproteinases 9
(MMP-9) gene expression were analyzed quantitatively. To elucidate the relationships between the
structural properties of flavonoids and their inhibitory activities, comparative molecular field analysis
and comparative molecular similarity indices analysis were carried out. The structural conditions
required for high inhibitory activity towards TNF-induced MMP-9 gene expression were derived.
In addition, for spiraeoside, which showed the best activity among the test compounds, reverse transcription
polymerase chain reaction (PCR), real-time PCR analysis, and promoter-reporter assay
were performed. Spiraeoside could be a lead compound for the anticancer agents.
Keywords: Matrix metallopeptidase 9, CoMFA, CoMSIA, flavonoid, spiraeoside.
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