Abstract: Over the past two decades, Methicillin-resistant Staphylococcus aureus (MRSA) has evolved from a controllable infectious disease into a serious public health concern. MRSA is largely a hospital-acquired infection and is, in fact, one of the most common. Recently, however, new strains have emerged in communities that are capable of causing severe infection in otherwise healthy persons. The antibacterial activity of five major compound is evaluate from Aristolochia brevipes (dichloromethane extract) as follows: (1) 9-methoxytariacuripyrone, (2) 7,9-dimethoxytariacuripyrone, (3) E/Z-N-formylnornantenine, (4) 6α-7-dehydro-N-formylnornantenine, (5) aristololactam I, (6) an amino compound which obtained by means of biotransformation (with Baker’s yeast), against Methicillin-sensitive Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA). The structures of these compounds were elucidated by 1H- and 13C- (one-dimension [1D] and two-dimension [2D]) Nuclear Magnetic Resonance (NMR) spectroscopy. The 9-methoxytariacuripyrone compounds and the compound obtained by biotransformation, 5-amino-9-methoxy-3,4-dihydro-2H-benzo(h)chromen-2-one,showed highest activity against MRSA strains at a concentration range of 4.0-16.0 μg mL-1. Hence, these compounds to hold promise as antibacterial agents in the treatment of infections with S. aureus, including MRSA and should be investigated further.