Platycodigenin is primarily known for its bioactive properties, especially in traditional and modern medicinal applications derived from Platycodon grandiflorum (balloon flower root). It exhibits significant anti-inflammatory effects by inhibiting pro-inflammatory cytokines and mediators, making it useful in managing inflammatory conditions. It also demonstrates potent antitumor activity, inducing apoptosis in various cancer cell lines, including lung, liver, and cervical cancers, through mitochondrial and caspase-dependent pathways.

The compound has been studied for its immunomodulatory effects, enhancing immune response by stimulating macrophage activity and cytokine production. Additionally, platycodigenin shows antiviral potential, particularly against respiratory viruses, by interfering with viral replication and entry into host cells. Traditionally, it is used to relieve respiratory symptoms such as cough and phlegm, supporting its role in respiratory health products.

Due to its saponin structure, it also acts as a natural surfactant, improving the absorption of other drugs, which makes it valuable in pharmaceutical formulations as an adjuvant. Its antioxidant properties further contribute to cellular protection against oxidative stress. Emerging research suggests hypoglycemic potential, which may support its development for diabetes management in nutraceuticals and functional health products.