Wang Yonglian, Jiang Shuxia, He Yaoxuan, Pang Ping, Shan Hongli
Shanghai Frontiers Science Research Center for Druggability of Cardiovascular Noncoding RNA, Institute for Frontier Medical Technology, School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201620, China.
Molecules. 2025 Apr 29;30(9):1972. doi: 10.3390/molecules30091972.
α-Lipoic acid (ALA) is a naturally occurring compound with diverse biological functions, widely distributed in animal and plant tissues. It has attracted considerable attention due to its versatile therapeutic potential. However, despite these promising prospects, the clinical application of ALA remains limited by its low bioavailability and chemical instability and an incomplete understanding of its multifaceted mechanisms across various diseases. This review provides a comprehensive overview of the biochemical properties of ALA, including its direct free-radical-scavenging activity, regeneration of endogenous antioxidants, chelation of metal ions, and modulation of inflammatory responses. We also highlight the current evidence regarding ALA's therapeutic roles and efficacy in major diseases, such as neurodegenerative disorders, lung diseases, cardiovascular diseases, and diabetes. Furthermore, recent advancements and innovative strategies in ALA-based derivatives and drug-delivery systems are summarized, emphasizing their potential to address complex diseases and the necessity for further translational studies. This review aims to provide a theoretical foundation for the rational design of ALA-based therapies, thereby supporting future clinical applications and the optimization of therapeutic strategies.
α-硫辛酸（ALA）是一种天然存在的化合物，具有多种生物学功能，广泛分布于动植物组织中。由于其具有多种治疗潜力，它已引起了相当大的关注。然而，尽管有这些前景广阔的方面，但ALA的临床应用仍然受到其低生物利用度、化学不稳定性以及对其在各种疾病中的多方面机制认识不全面的限制。本综述全面概述了ALA的生化特性，包括其直接清除自由基的活性、内源性抗氧化剂的再生、金属离子的螯合以及炎症反应的调节。我们还强调了关于ALA在主要疾病（如神经退行性疾病、肺部疾病、心血管疾病和糖尿病）中的治疗作用和疗效的当前证据。此外，总结了基于ALA的衍生物和药物递送系统的最新进展和创新策略，强调了它们应对复杂疾病的潜力以及进一步转化研究的必要性。本综述旨在为基于ALA的疗法的合理设计提供理论基础，从而支持未来的临床应用和治疗策略的优化。
