Carthamus tinctorius L. is commonly known as Safflower. C. tinctorius extracts and oil are important in drug development with numerous pharmacological activities in the world. This plant is cultivated mainly for its seed, which is used as edible oil. For a long time C. tinctorius has been used in traditional medicines as a purgative, analgesic, antipyretic and an antidote to poisoning. It is a useful plant in painful menstrual problems, post-partum hemorrhage and osteoporosis. C. tinctorius has recently been shown to have antioxidant, analgesic, anti-inflammatory and antidiabetic activities. Carthamin, safflower yellow are the main constituents in the flower of C. tinctorius. Carthamidin, isocarthamidin, hydroxysafflor yellow A, safflor yellow A, safflamin C and luteolin are the main constituents which are reported from this plant. Caryophyllene, p-allyltoluene, 1-acetoxytetralin and heneicosane were identified as the major components for C. tinctorius flowers essential oil. Due to the easy collection of the plant and being widespread and also remarkable biological activities, this plant has become both food and medicine in many parts of the world. This review presents comprehensive analyzed information on the botanical, chemical and pharmacological aspects of C. tinctorius.