Mangiferin, a C-glucopyranoside of 1, 3, 6, 7-tetrahydroxyxanthone, has been isolated from various parts of Mangifera indica (Anacardiaceae). The conclusive structure of mangiferin has been established by various researchers using a wide range of chemical and spectral analytical techniques. Mangiferin has been traditionally used in some parts of world as anti-inflammatory, analgesic, antipyretic, antioxidant, immunomodulator, antitumor, antiviral, and anthelminthic and in obesity treatment. The present article is an attempt to encompass various aspects and details related to the characterization of mangiferin and its subsequent pharmacological screening. The literature data on mangiferin has been comprehensively reviewed and evaluated by the authors and hence, the article contains brief description of phytochemical and pharmacological investigations conducted on mangiferin till now and thus may prove as a guiding force for further research in this particular area.