A search in ancient Chinese medicinal literature and modern phytochemical references indicates that the therapeutic value of Leonurus artemisia (I-mu ts'ao, the Chinese motherwort) might reside in a uterotonic principle present in leaves. Leonurine (4-guanidino-n-butyl syringate) was isolated from fresh and dry leaves of Leonurus artemisia. The uterotonic effect of leonurine was demonstrated in rat uterus in vitro. Results from this study suggest that functional phytochemistry based on ethnobotanical experience could lead to development of new and effective drugs from Chinese medicine.