Development of a Benzoxazine-derived Inhibitor Targeting Epithelial-to-Mesenchymal Transition in Lung Cancer.

BACKGROUND/AIM: The epithelial-to-mesenchymal transition (EMT) plays an essential role in lung cancer metastasis. This study aimed to explore the EMT inhibitory effect of the new compound 6,6'-(butylazanediyl) bis (methylene) bis (2,4-dimethylphenol) (2,4-diMBD).

MATERIALS AND

METHODS

Cell survival and proliferation were determined using cell viability and colony formation assays. Migration was analyzed using a wound-healing assay. The expression of proteins and mRNAs was examined using immunofluorescence assay and real-time quantitative PCR.

RESULTS

2,4-diMBD significantly suppressed colony formation and cell migration. In relation to its anti-migratory activity, we found that 2,4-diMBD decreased Snail, Slug, and zinc finger E-box binding homeobox (ZEB) levels at both the mRNA and protein levels, indicating EMT suppression in human lung cancer cells.

CONCLUSION

2,4-diMBD exerts anti-metastatic properties in lung cancer cells via EMT inhibition, and is a promising compound for the treatment of lung cancer.