Inhibitory Effect of Methyl Caffeate on Fos-Jun-DNA Complex Formation and Suppression of Cancer Cell Growth

摘要

The fos and jun proteins form a heterodimeric complex that interacts with the DNA regulatory element known as the AP-1 binding site. To search for inhibitors of the fos-jun-DNA complex formation, several natural plants extracts were screened. One of them, the methanol extract of Perilla frutescens showed inhibitory effect against the complex formation between the fos-jun dimer and the AP-1 binding site (TGAG/CTCA). Methyl caffeate and dibutyl phthalate (DBP) were isolated as the active constituents from the extract of P. frutescens by repeated column chromatography and HPLC. And their IC50 values for fos-jun-DNA complex formation were estimated as 0.29 mM and 0.55 mM, respectively. The more potent inhibitor, methyl caffeate showed cytotoxic effect against human cancer cell line (A549 and K562).