Abstract: From the clinical practices and summary of Chinese medicine， it has been proved that the discovery of lead compounds from natural medicine and followed by structural optimization toward innovative drugs is one of the most effective strategies for the modernization of Chinese medicine. A lot of research have exhibited that the chief pharmacological materials of single Chinese herb are always the naturally-abundant and structural featured constituent(s). In this perspective， we summarized the successful research stories of such constituents like artemisinin， arsenic trioxide and phlorizin， including discovery of the pharmacological activity， study of the molecular mechanism， structural optimization and development of innovative drugs. These experiences may contribute useful ideas for the researchers who are working in the field of drug discovery based on naturally abundant ingredients.