Impact of Icariin and its derivatives on inflammatory diseases and relevant signaling pathways

Herba Epimedii is a famous herb collected from China and Korea. It has been used for impotency, osteoporosis, and amnestic treatment for thousands of years. Icariin, a typical flavonoid compound isolated from Herba Epimedii, was reported as a potential anti-inflammatory drug. Icariside and icaritin are the two metabolites of icariin. Icariin and its metabolites have been used to treat a wide range of inflammatory diseases, such as atherosclerosis, Alzheimer’s disease, depression, osteoarthritis, and asthma. They exert powerful suppression of proinflammatory signaling, such as NF-κB and MAPKs. More importantly, they can upregulate anti-inflammatory signaling, such as GR and Nrf2. In this study, we review the therapeutic effects and mechanisms of icariin and its metabolites in inflammatory diseases and provide novel insights into these potential anti-inflammatory drugs.