Zhao Jiarui, Zhang Wei
College of First Clinical Medicine, Shandong University of Traditional Chinese Medicine, Jinan, Shandong, China.
Front Pharmacol. 2025 Jun 4;16:1619581. doi: 10.3389/fphar.2025.1619581. eCollection 2025.
Fibrosis is a pathological hallmark of various chronic diseases and contributes significantly to organ dysfunction and poor clinical outcomes. Despite the availability of antifibrotic agents, their limited efficacy and adverse side effect profiles underscore the urgent need for safer and more effective therapeutic alternatives. Traditional Chinese medicines have emerged as promising candidates for fibrosis management. , widely used in traditional Chinese medicine, exhibits notable antifibrotic activity, primarily attributed to its bioactive flavonoid icariin (ICA). However, the clinical application of ICA is hindered by its low bioavailability. Recent advances in extraction methods and drug delivery systems have improved the pharmacokinetic properties of ICA and related active metabolites, including icaritin and icariside II. These metabolites exert antifibrotic effects through multifaceted mechanisms, including anti-inflammatory and antioxidant activities, mitochondrial function modulation, apoptosis regulation, and autophagy. This review summarizes current insights into the molecular pathways through which ICA and related metabolites attenuate fibrosis, thereby supporting their potential for clinical translation in antifibrotic therapy.
纤维化是多种慢性疾病的病理标志，对器官功能障碍和不良临床结局有显著影响。尽管有抗纤维化药物，但它们有限的疗效和不良副作用凸显了对更安全、更有效治疗选择的迫切需求。中药已成为纤维化管理的有前景的候选药物。淫羊藿在传统中药中广泛应用，具有显著的抗纤维化活性，主要归因于其生物活性黄酮淫羊藿苷（ICA）。然而，ICA的临床应用因其低生物利用度而受到阻碍。提取方法和药物递送系统的最新进展改善了ICA及相关活性代谢物（包括淫羊藿次苷和淫羊藿苷II）的药代动力学性质。这些代谢物通过多方面机制发挥抗纤维化作用，包括抗炎和抗氧化活性、线粒体功能调节、凋亡调控和自噬。本综述总结了目前对ICA及相关代谢物减轻纤维化的分子途径的见解，从而支持它们在抗纤维化治疗中临床转化的潜力。
