Crocus sativus L. (C. sativus), commonly known as saffron, is used as a food additive, preservative, and medicinal herb. Traditionally, it has been used as an alternative treatment for different diseases. C. sativus' medicinal effects are related to its major constituents like crocins, crocetin, and safranal. According to the literature, C. sativus and its constituents could be considered as an effective treatment for neurodegenerative disorders, coronary artery diseases, asthma, bronchitis, colds, fever, diabetes, and so on. Recently, numerous studies have reported such medicinal properties and found that the underlying mechanisms of action may be mediated by antioxidant, inflammatory, and immunomodulatory effects. C. sativus enhances the antioxidant capacity and acts as a free radical scavenger. As an antiinflammatory and immunomodulatory agent, it modulates inflammatory mediators, humoral immunity, and cell-mediated immunity responses. This review highlights in vitro and animal findings regarding antiinflammatory, antioxidant, and immunomodulatory effects of C. sativus and its constituents. Present review found that the C. sativus and its main constituents such as safranal, crocins, and crocetin could be effective against various diseases because of their antioxidant, anti-inflammation, and immunomodulatory effects. Copyright © 2016 John Wiley & Sons, Ltd.