Traditional Chinese Medicine College of Shandong University of Traditional Chinese Medicine, Jinan, China.
Department of Pneumology, Affiliated Hospital of Shandong University of Traditional Chinese Medicine, Jinan, China.
Biomed Pharmacother. 2022 Jul;151:113180. doi: 10.1016/j.biopha.2022.113180. Epub 2022 May 27.
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.
近年来，由于炎症和免疫失调在许多疾病的病理生理学中发生，因此受到了广泛关注。在这方面，已经进行了几项药理学研究，旨在评估植物化学物质的潜在抗炎和免疫调节作用。中药淫羊藿常被用作补品、壮阳药和抗风湿药。淫羊藿苷（ICA）是淫羊藿的主要活性成分，摄入后主要代谢为淫羊藿次苷（ICT）。体外和体内研究数据表明，ICA 及其代谢物（ICT）调节免疫细胞的功能和激活，调节炎症因子的释放，并恢复异常信号通路。ICA 和 ICT 还参与了几种疾病的抗炎和免疫反应，包括多发性硬化症、哮喘、动脉粥样硬化、狼疮性肾炎、炎症性肠病、类风湿关节炎和癌症。然而，数据表明 ICA 和 ICT 表现出相似但不完全相同的药代动力学特性。因此，基于它们更高的溶解度和生物利用度，以及表明单一组分化合物具有更广泛和更安全的治疗能力的趋势，ICA 和 ICT 传递系统和治疗代表了具有广阔前景的临床应用的有趣途径。在这项研究中，我们综述了 ICA 及其代谢物 ICT 的抗炎和免疫调节机制以及药代动力学特性。
