Through the analysis on domestic and foreign literature reports, the pharmacological actions and mechanisms, pharmacokinetics and clinical application of platycodin are reviewed. Platycodin is considered to be the main effective component of platycodon. It shows significant activity of anti-tumor, and the mechanism involves inhibiting tumor cell proliferation and pathological angiogenesis, inducing tumor cell apoptosis and autophagy, inhibiting tumor cell migration, adhesion and invasion and so on. In addition, it also shows the effects of immune regulation, anti-inflammation, liver protection and anti-atherosclerosis. Pharmacokinetic studies have showed that the oral bioavailability of platycodin is poor, and the metabolism in vivo is affected by intestinal flora and compatibility. In clinic, the application of prescriptions consisting of platycodon as the main drug shows better efficacy in the treatment of respiratory diseases, lung cancer, breast cancer and other malignant tumors.