A highly reliable high-performance liquid chromatography method was developed and validated for determining quality of extracts from the leaves of Dipsacus sativus (Linn.) Honck. Under optimum conditions, the chromatography profile of eight compounds was collected, with compound saponarin as marker. The analysis results indicated that saponarin and isovitexin were the main active components.Pharmacological experiments proved that extracts from the leaves showed significant antioxidant activity. This work could serve to validate the usefulness of high-performance liquid chromatography analyses in traditional Chinese medicine.