Saikosaponins are the main active ingredients of Bupleurum chinense, including five subtypes:protoglycoside, homoannular diene, heteroannular diene, oleanolic acid and △¹² oleanane. Saikosaponins have strong anti-inflammatory activities. In vivo studies have shown that saikosaponins can effectively alleviate inflammatory diseases and reduce the expression of pro-inflammatory cytokines, mainly by inhibiting the nuclear factor-κB signaling pathway. Saikosaponins have antioxidant activities. It can significantly reduce the levels of reactive oxygen species and malondialdehyde which is one of the lipid peroxidation products, and enhance the activities of antioxidant enzymes such as superoxide dismutase, catalase and glutathione peroxidase. Saikosaponins may also have lipid-lowering effects. Based on the roles of saikosaponins in anti-inflammation, anti-oxidation and lipid-lowering effects, saikosaponins are expected to be used in the prevention and treatment of atherosclerosis.