Bioassay-guided fractionation of the MeOH extract of Ephedra sinica terrestrial stems, using a PPAR-γ ligand binding assay, resulted in the isolation of 10 compounds, including one new bisabolane-type sesquiterpenoid (10). The structure of the new compound was determined by extensive spectroscopic analysis, including two-dimensional (2D) NMR. Among the isolated compounds, the sitosterol derivatives (1 and 2), flavonoid glucoside (7), and the new sesquiterpenoid (10), showed significant PPAR-γ ligand-binding activity.