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天然产物磷酸化研究进展。

Progress in phosphorylation of natural products.

机构信息

Key Laboratory of Therapeutic Substance of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China.

Department of Pharmacy, Characteristic Medical Center of PAP, Tianjin, 300162, China.

出版信息

Mol Biol Rep. 2024 May 27;51(1):697. doi: 10.1007/s11033-024-09596-1.

Abstract

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.

摘要

天然药物是开发新药的宝贵资源。然而,某些成分溶解度低和生物利用度差等因素限制了它们作为药物的疗效和潜力。天然产物的结构修饰已成为药物开发的一个重要研究领域。磷酸化基团作为重要的内源性活性基团,已广泛应用于基于天然分子的结构修饰和新药开发。将磷酸基团引入天然分子不仅可以提高其稳定性、生物利用度和药理学性质,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。本综述总结了天然药物的磷酸化机制、修饰方法和生物活性增强作用。值得注意的是,多糖、类黄酮、萜类、蒽醌和香豆素等化合物经磷酸化修饰后,抗氧化、抗癌、抗病毒、免疫调节、抗衰老、酶抑制、抑菌、保肝和降血脂等作用增强。

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