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Natural products with high pharmacological potential and low toxicity have been considered as the novel therapeutic agents. Crocetin is an active constituent of saffron (Crocus sativus L.) stigma, which in its free-acid form is insoluble in water and most organic solvents. Crocetin exhibits various health-promoting properties including anti-tumor, neuroprotective effects, anti-diabetics, anti-inflammatory, anti-hyperlipidemia, etc. These therapeutic effects can be achieved with different mechanisms such as improvement of oxygenation in hypoxic tissues, antioxidant effects, inhibition of pro-inflammatory mediators, anti-proliferative activity and stimulation of apoptosis in cancer cells. It is also worth considering that crocetin could be tolerated without major toxicity at therapeutic dosage in experimental models. In the present review, we discuss the biosynthesis, pharmacokinetic properties of crocetin and provide a …