The invention relates to a setwall extract with hypnotic sedative activity and the preparation thereof and also comprises the application of the extract in the pharmacy field. The extract essentially consists of setwall naphtha, valerienic acid, total valepotriate, etc. The pharmacodynamical experiment shows that the setwall extract made by the technology has the marked pharmacological actions of mitigation, hypnosis, anti-depression, spasmolysis, analgesis, the regulation of blood fat, anti-tumor, antibiosis, antivirus and the like and can be developed into medicine or food with health care function.