Cholestasis is a clinical syndrome withretention of excessive toxic bile acids that causes liver injury.Varieties of nuclear receptors, metabolizing enzymes and transporters play crucial roles in bile acid metabolism and elimination.Appropriate regulation of bile acid homeostasis is critically important for protection against cholestatic liver injury.Herbal medicines and natural products have been used extensively for protection against liver injury.In this presentation, using Schisandra sphenanthera and Schisandrol B as examples, on the basis of metabolomic analysis of bile acids, the hepato-protection of these compounds in WT and KO mice, the important role of PXR-regulated enzymes and transporters in their hepato-protection, and evidences on their PXR activation in vitro will be illustrated and discussed.