Inflammation and immunity dysregulation have received widespread attention in recent years due to their occurrence in the pathophysiology of many conditions. In this regard, several pharmacological studies have been conducted aiming to evaluate the potential anti-inflammatory and immunomodulatory effects of phytochemicals. Epimedium, a traditional Chinese medicine, is often used as a tonic, aphrodisiac, and anti-rheumatic agent. Icariin (ICA) is the main active ingredient of Epimedium and is, once ingested, mainly metabolized into Icaritin (ICT). Data from in vitro and in vivo studies suggested that ICA and its metabolite (ICT) regulated the functions and activation of immune cells, modulated the release of inflammatory factors, and restored aberrant signaling pathways. ICA and ICT were also involved in anti-inflammatory and immune responses in several diseases, including multiple sclerosis, asthma, atherosclerosis, lupus nephritis, inflammatory bowel diseases, rheumatoid arthritis, and cancer. Yet, data showed that ICA and ICT exhibited similar but not identical pharmacokinetic properties. Therefore, based on their higher solubility and bioavailability, as well as trends indicating that single-ingredient compounds offer broader and safer therapeutic capabilities, ICA and ICT delivery systems and treatment represent interesting avenues with promising clinical applications. In this study, we reviewed the anti-inflammatory and immunomodulatory mechanisms, as well as the pharmacokinetic properties of ICA and its metabolite ICT.


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