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Abstract: Ethnopharmacological relevance: Carthamus tinctorius L. (Compositae), a widely used traditional Chinese medicine, was known as Hong hua (Chinese: ▪), safflower. Safflower with a wide spectrum of pharmacological effects has been used to treat dysmenorrhea, amenorrhea, postpartum abdominal pain and mass, trauma and pain of joints, etc. The present paper reviews the advancements in investigation of botany and ethnopharmacology, phytochemistry, pharmacology and toxicology of safflower. Finally, the possible tendency and perspective for future investigation of this plant are discussed, too. Materials and methods: The information on safflower was collected via piles of resources including classic books about Chinese herbal medicine, and scientific databases including Pubmed, Google Scholar, ACS, Web of science, CNKI and others. Results: Over 104 compounds from this plant have been isolated and identified, and quinochalcones and flavonoids are considered as the characteristic and active constituents of safflower. Safflower with its active compounds possesses wide-reaching biological activities, including dilating coronary artery, improving myocardial ischemia, modulating immune system, anticoagulation and antithrombosis, antioxidation, antiaging, antihypoxia, antifatigue, antiinflammation, anti-hepatic fibrosis, antitumor, analgesia, etc. Conclusions: As an important traditional Chinese medicine, it is important to investigate the pharmacological effects and molecular mechanisms of this plant based on modern realization of diseases' pathophysiology. More bioactive components should be identified using bioactivity-guided isolation strategies, and the possible mechanism of action as well as potential synergistic or antagonistic effects of multi-component mixtures derived from safflower need to be evaluated integrating pharmacological, pharmacokinetic, bioavailability-centered and physiological approaches. Further studies on safflower can lead to the development of new drugs and therapeutics for various diseases, and how to utilize it better should be paid more attention to. [ABSTRACT FROM AUTHOR]