[Objective] This study aimed to isolate and identify the chemical con- stituents of Selaginella tamariscina. [Method] The chemical compounds isolated from the whole plant of traditional Chinese herb S. tamariscina were purified through col- umn chromatography and preparative thin-layer chromatography, and then chemical structures of the compounds were determined by NMR and mass spectrometry. Fi- nally, the anticancer activity of the compounds 5, 6 and 7 was measured by MTT assay. [Result] Seven compounds, containing carnaubic acid （1）, glucose （2）, [3-sitos- terol （3）, amentoflavone （4）, selaginellin （5）, selaginellin M （6） and selaginellin A （7）, were isolated from methanol extracts of S. tamariscina. Among the three tested compounds, compound 7 exhibited the most effective activity to inhibit the HeLa cell growth. [Conclusion] This study will provide a basis for better development and uti- lization of Selaginella plant resources.