Anti-inflammatory and immunoregulatory effects of icariin and icaritin.

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.

A comprehensive review of tanshinone IIA and its derivatives in fibrosis treatment.

Tanshinone IIA (Tan IIA) is the most abundant lipid-soluble component in Salvia miltiorrhiza. Both Tan IIA and its derivatives including Sodium tanshinone IIA sulfonate (STS) have been widely used in clinic due to their proved anti-inflammation, anti-oxidation, and anti-fibrosis functions. Recently, combinations containing Tan IIA and active components have attracted intensive interest in fibrosis. Multiple studies have been conducted to attempt to decipher the mechanisms of this traditional Chinese medicine and found that Tan IIA can attenuate fibrosis through different pathways such as Smad2/3, NF-κB, Nrf2, E2F and snail/twist axis. However, some of the studies were contradictory and confusing. Therefore, it was important to develop an easy-to-access reference for clinic use. In this study, we reviewed the pharmacological mechanisms, pharmacokinetics, and toxicology of Tan IIA and its derivatives in the treatment of fibrosis and introduced the cutting-edge new formulation of Tan IIA compound.