Platycodon grandiflorum contains various chemical components, including saponins, flavonoids, phenolic compounds, and polysaccharides, among which saponins are the main active substances. Extensive research has been conducted both in China and abroad on the efficacy mechanisms and pharmacological activities of P. grandiflorum saponins. These studies have found that P. grandiflorum saponins exhibit significant health benefits, including cough suppression, asthma relief, liver protection, anti-tumor effects, antioxidant properties, and anti-inflammatory and analgesic actions. This article provides a review of the chemical composition and structure, extraction and purification methods, as well as the efficacy of P. grandiflorum saponins. It also discusses the current state of research on P. grandiflorum saponins and offers prospects for future research directions.