The effects of crude extract and bioactive fractions from Brachyglottis monroi on biological activity were investigated. The crude ethanol extract inhibited the growth of the Gram positive bacterium Bacillus subtilis (ATCC Strain number 19659, 1 mm zone at 150 μg/disk) and the dermatophyte Trichophyton mentagrophytes (ATCC 28185, 2 mm zone at 150 μg/disk), and toxic to P388 tumor cells (IC50 23.96 μg/ml at 75 μg/disk). Cytotoxic activity was strongly showed by Fr. 6 (P388 IC50 19.67 μg/ml at 75 μg/disk).