For many years, plants have been used in the traditional medicine of different cultures. The biennial plant of the family Asteraceae, Onopordum acanthium L., also known as Scotch thistle, is used in traditional medicine as an anti-inflammatory, antitumor, and cardiotonic agent. The plant is widespread in the world; it grows in Europe and Asia and was introduced to America and Australia. Stems and buds of the first-year plant are used in cooking as an analogue of artichoke in European cuisine. Additionally, inflorescences contain a complex of proteolytic enzymes “onopordosin„, which may be used as a milk-clotting agent in the dairy industry. The chemical composition of the aerial part and roots of O. acanthium is represented by flavonoids, phenylpropanoids, lignans, triterpenoids, sesquiterpene lactones, and sterols. The anti-inflammatory, antiproliferative, and cardiotonic properties of the plant have been confirmed by pharmacological experiments with extracts and individual compounds using in silico, in vitro, and in vivo methods. This work is a review of information on the chemical composition and pharmacological studies of O. acanthium as a promising medicinal plant.