Isolupalbigenin shows promising cytotoxic effects toward HL-60 cells (IC50 4.3 ± 0.7 to 18.0 ± 1.7 uM), it also shows in vitro inhibitory activity toward human glyoxalase I. Isolupalbigenin shows two different antibacterial activities against MRSA: direct growth inhibition and intensification of methicillin sensitivity, it could lead to the development of compounds for new approaches against MRSA infection.