Saffron (Crocus sativus L. stigma), the most valuable medicinal food product, belongs to the Iridaceae family which has been widely used as a coloring and flavoring agent. These properties are basically related to its crocins, picrocrocin and safranal contents which have all demonstrated health promoting properties. The present review article highlights the phytochemical constituents (phenolic and flavonoid compounds, degraded carotenoid compounds crocins and crocetin) that are important in antioxidant activity of saffron extracts. However, the synergistic effect of all the bioactive components presence in saffron gave a significant antioxidant activity similar to vegetables rich in carotenoids. Our study provides an updated overview focused on the antioxidant activity of saffron related to its bioactive compounds to design the different functional products in food, medicine and cosmetic industries.