The occurrence of vancomycin-resistant Staphylococcus aureus (VRSA) and multidrug-resistant (MDR) strains of this organism necessitate the discovery of new classes of anti-staphylococcal drug leads. At present there are no single chemical entity plant derived antibacterials used clinically, and this biologically diverse group deserves consideration as a source of chemical diversity for two important reasons. Firstly, plants have exceptional ability to produce cytotoxic agents and, secondly, there is an ecological rationale that antibacterial natural products should be present or synthesised de novo following microbial attack to protect plants from invasive and pathogenic microbes in their environment. This review cites plant natural products that either modify resistance in Staphylococcus aureus or are antibacterial through bacteriostatic or bactericidal properties. The activities described here show that there are many potential new classes of anti-staphylococcal agents which should undergo further cytotoxicity, microbial specificity and preclinical in vivo studies to assess their potential.