Three known ${alpha}$-amyrin triterpenoids, ursolic acid (1), $2{alpha},3{alpha}$-dihydro xyurs-12-ene-28-oic acid (2) and euscaphic acid (3), and ${eta}$-amyrin triterpenoid, $3{eta}$-hydroxyolean-5,12-diene (4), and ${alpha}$-spinasterol (5) have been isolated from the fractionated n-butanol extracts of the spikes of Prunella vulgaris var. lilacina, guided by DNA topoisomerases I and II inhibitory activities and cytotoxic activity against human cancer cells. Their structures were elucidated on the basis of spectroscopic and chemical methods. Compound 4 exhibited significant cytotoxic activity against human colon adenoblastoma (HT-29), and 5 showed DNA topoisomerase I and II inhibitions.