Ten new triterpenoids, including nine 9,10-seco-cycloartanes (1-9) and one 9,19-cyclolanostane (10), as well as one sesquiterpenoid (11) and four known compounds (12-15), were extracted and purified from the whole plant of the Chinese liverwort Lepidozia reptans. Multiple techniques (NMR, HRESIMS, IR, and X-ray crystallographic analysis) were applied to determine the structures of the isolated compounds. Bioassay determinations showed that compound 7, which contains an α,β-unsaturated carbonyl moiety in its structure, inhibited the growth of a panel of cancer cell lines with IC50 values ranging from 4.2 ± 0.2 to 5.7 ± 0.5 μM. Further investigation revealed that compound 7 induces PC-3 cell death via mitochondrial-related apoptosis.