Arctium lappa (family, Asteraceae), commonly called Burdock, owing to its diverse volatile and nonvolatile metabolites is known for a variety of therapeutic and pharmacological effects. These secondary metabolites consist of phytosterols, terpenes/terpenoids, hydrocarbons, flavonoids, fatty acids, carboxylic derivatives, lignans, fatty acids, acetylenic compounds, polysaccharides, aldehydes, methoxypyrazines, carboxylic and fatty acids, monoterpenes, and sesquiterpenes. Burdock has also shown multifaceted pharmacological actions that include antidiabetic, antioxidant, hepatoprotective, anticancer, gastroprotective, antibacterial, antiallergic, antimicrobial, antiviral, and anti-inflammatory. This chapter aims to provide a comprehensive overview of the chemistry and biological activities of the secondary metabolites found in A. lappa and its species.