Abstract: Asterric acid and its derivatives,possessing a diphenyl ether structure,were isolated from a number of Aspergillus and Penicillium species’ culture.They exhibited good or excellent medicinal activity and pesticide activity such as antifungal,antibacterial,cytototoxic activity,fungicidal activity,nematicidal activity and seed germination inhibition of water dropwort and so on.In particularly,asterric acid as an inhibitor of vascular endothelial growth factor (VEGF) has commercialized as biochemical reagent and was applied to the studies on biology and medicine.The advances in the isolation,structures and biological activity of asterric acid and its derivatives have been reviewed.Their biosynthetic and metabolic mechanism,total synthesis and structure modification have been also introduced.