天然药物是新药开发的宝贵资源。然而，某些成分的低溶解度和生物利用度差等因素阻碍了它们作为药物的功效和潜力。天然产物的结构修饰已成为药物开发的重要研究领域。磷酸化基团作为重要的内源活性基团，已被广泛用于基于天然分子的结构修饰和新药物的开发。将磷酸基团引入天然分子中不仅可以增强其稳定性、生物利用度和药理特性，还可以通过改变其电荷、氢键和空间结构来提高其生物活性。本文综述了天然药物的磷酸化机制、修饰方法以及增强生物活性的研究。值得注意的是，多糖、类黄酮、萜类化合物、蒽醌和香豆素等化合物在磷酸化修饰后表现出增强的抗氧化、抗癌、抗病毒、免疫调节、抗衰老、酶抑制、抑菌、保肝和降脂作用。© 2024。作者(s)，获得 Springer Nature B.V. 的独家许可。

Natural medicines are a valuable resource for the development of new drugs. However, factors such as low solubility and poor bioavailability of certain constituents have hindered their efficacy and potential as pharmaceuticals. Structural modification of natural products has emerged as an important research area for drug development. Phosphorylation groups, as crucial endogenous active groups, have been extensively utilized for structural modification and development of new drugs based on natural molecules. Incorporating phosphate groups into natural molecules not only enhances their stability, bioavailability, and pharmacological properties, but also improves their biological activity by altering their charge, hydrogen bonding, and spatial structure. This review summarizes the phosphorylation mechanism, modification approaches, and biological activity enhancement of natural medicines. Notably, compounds such as polysaccharides, flavonoids, terpenoids, anthraquinones, and coumarins exhibit increased antioxidation, anticancer, antiviral, immune regulatory, Antiaging, enzyme inhibition, bacteriostasis, liver protection, and lipid-lowering effects following phosphorylation modification.© 2024. The Author(s), under exclusive licence to Springer Nature B.V.