Lobetyolin is a polyacetylene glycoside, a type of natural product characterized by its structure containing an acetylenic bond and a glucose moiety. It is a major bioactive constituent isolated from the roots of *Codonopsis pilosula* (Dangshen), a plant widely used in traditional Chinese medicine. Its primary application is in the field of pharmaceutical research and natural product-based therapeutics. Studies have shown that lobetyolin possesses various pharmacological activities, including anti-inflammatory, antioxidant, immunomodulatory, and gastroprotective effects. It is considered a key marker compound for the quality control of *Codonopsis* species and is investigated for its potential in developing treatments for conditions related to inflammation, immune dysfunction, and digestive disorders. As a defined phytochemical, lobetyolin serves as a reference standard in analytical chemistry for the authentication and standardization of herbal medicines. Its research use is centered on exploring the mechanistic basis of traditional herbal remedies and evaluating its potential as a lead compound for new drug development.