天麻素是天麻中的主要药理活性成分之一，具有镇静、镇痛、降压等作用。天麻素脂溶性低、在体内代谢快等问题限制了其应用。然而，天麻素本身具有相对分子质量低、羟基含量高和化学结构易修饰等特点，使其具有极大的药物开发潜力。因此，对天麻素进行结构修饰从而获得具有更佳药理活性的天麻素衍生化合物一直是研究热点。通过从天麻素结构修饰的合成路线方面归纳总结了天麻素的简单乙酰化、席夫碱修饰，酯化、酰胺化、芳基取代分子拼接修饰，聚氨酯交联高分子材料嵌合修饰等不同结构修饰方式。为以天麻素结构修饰作为基础的新衍生物、新药、新材料的深入研究提供参考。

Gastrodin is one of the main pharmacologically active components in Tianma (Gastrodiae Rhizoma), with effects such as sedative, analgesic, and antihypertensive properties. However, its low lipid solubility and rapid metabolism in the body limit its application. Despite these challenges, gastrodin possesses characteristics such as a low molecular weight, high hydroxyl content, and a chemical structure that is easily modified, which give it great potential for drug development. Therefore, structural modification of gastrodin to obtain derivatives with improved pharmacological activities has been a hot research topic. This review summarizes various structural modification approaches for gastrodin, including simple acetylation, Schiff base modification, esterification, amidation, aryl substitution molecular conjugation, and polyurethane cross-linked polymer material embedding. This provides a reference for further research on new derivatives, drugs, and materials based on the structural modification of gastrodin.

R284

陕西省重点研发项目（2024NC-YBXM-182）;陕西省教育厅重点科学研究计划项目（23JY017）;陕西理工大学“市校共建”科研专项（SXC-2301）