Identification and biological evaluation of natural product Biochanin A

Natural products have shown promise for epigenetic modulations and thus are therapeutically potential for cancer prevention and treatment. In this work, we report the identification of natural product Biochanin A as a new LSD1 inhibitor and further biological evaluation in gastric MGC-803 cells. Biochanin A effectively and reversibly inhibited LSD1 (IC50 = 2.95 μM) and showed selective inhibition to LSD1 over MAO-A/B. In gastric MGC-803 cells, Biochanin A induced accumulation of H3K4me1/2, inhibited cell growth moderately (IC50 = 6.77 µM), but was less toxic to normal GES-1 (IC50 > 32 µM). Mechanistic studies showed that Biochanin A suppressed colony formation, cell apoptosis, and migration of MGC-803 cells. This study may help to elucidate the anticancer mechanisms of Biochanin A.