Asteraceae is a large family of flowering plants known as Angiospermae. Asteraceae provides coffee substitutes, herbal teas, sweetening agents, artichokes, sunflower seeds, leaf vegetables, and cooking oils. Plants of Asteraceae with commercial importance include Lactuca sativa, Cynara cardunculus, Carthamus tinctorius (safflower), Smallanthus sonchifolius, Helianthus annuus (sunflower), and so on. Many bioactive compounds including essential oils, polysaccharides, flavonoids, clerodane-type diterpenes, triterpenoid saponines, phenols, salicylic acid derivatives, occur in Asteraceae, and have many biological activities, such as gastroprotective, antioxidant, cytotoxic, anti-obesity, anti-inflammatory, spasmolytic, and antimicrobial effects. Diuretic activities have been linked with leiocarposide and flavonoids, while anti-inflammatory effects are attributed to phenolic compounds such as leiocarposide, hyperoside, quercitrin, and so on. Cytotoxic activities could be attributed to the terpenic compounds. The energy store in Asteraceae mostly exists as inulin. Asteraceae produces tannins, acetylenes, alkaloids, iso/chlorogenic acid, pentacyclic triterpene alcohols, sesquiterpene lactones, and so on. Most of the substances have promising potential in medicine, diet, and therapeutics. © 2023 Scrivener Publishing LLC. All rights reserved.