Cardoon (Cynara cardunculus L.) is a Mediterranean plant and member of the Asteraceae family that includes three botanical taxa, the wild perennial cardoon (C. cardunculus L. var. sylvestris (Lamk) Fiori), globe artichoke (C. cardunculus L. var. scolymus L. Fiori), and domesticated cardoon (C. cardunculus L. var. altilis DC.). Cardoon has been widely used in the Mediterranean diet and folk medicine since ancient times. Today, cardoon is recognized as a plant with great industrial potential and is considered as a functional food, with important nutritional value, being an interesting source of bioactive compounds, such as phenolics, minerals, inulin, fiber, and sesquiterpene lactones. These bioactive compounds have been vastly described in the literature, exhibiting a wide range of beneficial effects, such as antimicrobial, anti-inflammatory, anticancer, antioxidant, lipid-lowering, cytotoxic, antidiabetic, antihemorrhoidal, cardiotonic, and choleretic activity. In this review, an overview of the cardoon nutritional and phytochemical composition, as well as its biological potential, is provided, highlighting the main therapeutic effects of the different parts of the cardoon plant on metabolic disorders, specifically associated with hepatoprotective, hypolipidemic, and antidiabetic activity.