The chemical groups isolated from Carthamus tinctorius were included oils, proteins, minerals, phenolics, flavonoids, alkaloids, lignans, carboxylic acids, steroids, polysaccharides, quinochalcone C-glycosides and quinone-containing chalcones. It exerted many pharmacological activities including central nervous, cardiac, vascular, anticoagulant, reproductive, gastrointestinal, antioxidant, hypolipidemic, metabolic and many other pharmacological effects. This paper will highlight the chemical constituents and pharmacological effects of Carthamus tinctorius.