The root of L. has been shown to possess anti-gout and anti-diabetic properties, but the compounds responsible for these pharmaceutical effects have not yet been reported. In this study, we aimed to isolate and purify active components from the root of , and to evaluate their anti-radical, anti-gout and anti-diabetic capacities. From the ethyl acetate (EtOAc) extract, two compounds, chrysophanol () and physcion (), were isolated by column chromatography with an elution of hexane and EtOAc at a 9:1 ratio. Their structures were identified by spectrometric techniques including gas chromatography-mass spectrometry (GC-MS), electrospray ionization-mass spectrometry (ESI-MS), X-ray diffraction analyses and nuclear magnetic resonance (NMR). The results of bioassays indicated that () showed stronger activities than (). For antioxidant activity, () and () exhibited remarkable DPPH radical scavenging capacity (IC = 9.8 and 12.1 µg/mL), which was about two times stronger than BHT (IC = 19.4 µg/mL). The anti-gout property of () and () were comparable to the positive control allopurinol, these compounds exerted strong inhibition against the activity of xanthine oxidase (IC = 36.4 and 45.0 µg/mL, respectively). In the anti-diabetic assay, () and () displayed considerable inhibitory ability on α-glucosidase, their IC values (IC = 20.1 and 18.9 µg/mL, respectively) were higher than that of standard acarbose (IC = 143.4 µg/mL). Findings of this study highlight that () and () may be promising agents to treat gout and diabetes, which may greatly contribute to the medicinal properties of root.