Antineoplastic effects of icaritin: molecular mechanisms and applications

Icaritin (ICA) is a prenylflavonoid natural product extracted from plants of the Epimedium genus. The approval of ICA softgel capsules as a class 1.2 traditional Chinese medicine (TCM) innovative drug represents a major advancement offering a novel therapeutic approach for patients with advanced hepatocellular carcinoma (HCC). Class 1.2 TCM innovative drugs generally denote extracts and formulations derived from single plants, animals, minerals, or other substances. ICA exhibits diverse pharmacological effects, encompassing anti-inflammatory, immune-regulatory, anti-oxidation, anti-osteoporosis, anti-depression, and notably anti-cancer properties. This review presents a comprehensive overview of the molecular mechanisms underlying the anti-cancer properties of ICA, and further highlights recent progress in use of ICA in cancer research, discusses present challenges, and examines potential opportunities for ICA application and further development.