Objective To investigate the chemical constituents of Artemisia capillaris, traditional Chinese herb, with a view to discovering the lead compounds with pharmacological activities. Methods The chemical constituents were isolated and purified by the combination of macroporous adsorption resin, silica gel, ODS column chromatography and semi-preparative high performance liquid chromatography. The structures of the isolates were identified based on the physico-chemical properties and NMR spectroscopy data. In addition, the anti-hepatocellular carcinoma and anti-HBV activities of the isolated compounds were tested by MTT assay and ELISA. Results Ten compounds were isolated from the ethanol extract of Artemisia capillaris. Bioassay screening indicated that those isolates were not active. Conclusion Compounds 1 and 2 were new compounds, compounds 1, 3, and 4 are polyacetylenes, compounds 2 and 10 are aliphatic acid, and compounds 5-9 are terpenoids.