Six compounds including three new benzophenones, selagibenzophenones D-F (1–3), two known selaginellins (4–5) and one known flavonoid (6), were isolated fromSelaginella tamariscina. The structures of new compounds were established by 1D-, 2D-NMR and HR-ESI-MS spectral analyses. Compound1represents the second example of diarylbenzophenone from natural sources. Compound2possesses an unusual biphenyl-bisbenzophenone structure. Their cytotoxicity against human hepatocellular carcinoma HepG2 and SMCC-7721 cells and inhibitory activities on lipopolysaccharide-induced nitric oxide (NO) production in RAW264.7 cells were evaluated. Compound2showed moderate inhibitory activity against HepG2 and SMCC-7721 cells, and compounds4and5showed moderate inhibitory activity to HepG2 cells. Compounds2and5also exhibited inhibitory activities on lipopolysaccharide-induced nitric oxide (NO) production.