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Bacterial resistance to antibiotics is a serious global problem and includes strains of beta-lactam-resistant Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Novel antimicrobials and/or new approaches to combat the problem are urgently needed. The Chinese herb Xi-nan Huangqin (Scutellaria amoena C.H. Wright) has been used in traditional Chinese medicine to treat a wide range of infectious diseases. In this study we have examined the antibacterial action of baicalin, a flavone isolated from the herb. When combined with 16 microg mL(-1) baicalin, minimum inhibitory concentrations (MICs) of benzylpenicillin against MRSA and penicillin-resistant S. aureus were reduced from 125 and 250 microg mL(-1) to 4 and 16 microg mL(-1), respectively. This activity of baicalin was dose-dependent. Viable counts showed that the killing of MRSA and beta-lactam-resistant S. aureus cells by 10 to 50 microg mL(-1) ampicillin, amoxycillin, benzylpenicillin, methicillin and cefotaxime was potentiated by 25 microg mL(-1) baicalin. From the study it was concluded that baicalin has the potential to restore the effectiveness of beta-lactam antibiotics against MRSA and other strains of beta-lactam-resistant S. aureus. In view of its limited toxicity baicalin offers potential for the development of a valuable adjunct to beta-lactam treatments against otherwise resistant strains of microorganisms.