Novel bakuchiol derivatives inhibit the migration and invasion of non-small cell lung cancer by suppressing epithelial-to-mesenchymal transition

Abstract

Recently, bakuchiol and its derivatives have been widely investigated owing to their anticancer activity. However, there are few studies on the inhibition of epithelial–mesenchymal transition (EMT) by bakuchiol and its derivatives. Besides, thiosemicarbazones (TSCs) have also been demonstrated to exhibit potential EMT-inhibitory effects. Hence, the cytotoxic activity of novel bakuchiol derivatives containing thiosemicarbazone moieties was evaluated against two non-small lung cancer cell lines. Among them, compound 2f demonstrated the highest activity, with IC₅₀ values of 2.23 and 5.55 µM against PC9 and H1975 cells, respectively. Compound 2f effectively suppresses tumor cell proliferation by inducing cell cycle arrest and promoting apoptosis. Additionally, various evidence after treatment with compound 2f in PC9 cells, including the inhibition of migration and invasion, the enhancement of E-cadherin expression and reduction of vimentin levels, indicated the role of bakuchiol derivatives in inhibiting EMT. These findings suggest that bakuchiol derivatives could be positioned as potential candidates for cancer treatment.