Harpagoside, a major iridoid glycoside present in Harpagophytum procumbens (devil's claw), has been reported to show antiinflammatory, anti-rheumatic, and analgesic activities. The present study is aimed to provide a comprehensive overview of antiinflammatory activity of harpagoside. Peer-reviewed articles on potent anti-inflammatory effects of harpagoside were acquired from Scopus, ScienceDirect, and SciFinder. This review provides a comprehensive advance on the pharmacological studies to confirm potent anti-inflammatory effects of harpagoside in vitro, in vivo, and clinical studies. Although a number of researches have demonstrated anti-inflammatory activities of harpagoside, further intensive studies are required to confirm its efficacy for treating inflammatory diseases as a therapeutic agent.