[关键词]
[摘要]
黄芪多糖(Astragalus polysaccharides,APS)是黄芪的主要活性成分,具有多种药理活性,但因其高相对分子质量、低溶解性导致生物利用度较低,限制了其临床应用。硒化修饰可有效改善其理化特性及生物活性,形成硒化黄芪多糖(Se-APS)和黄芪多糖纳米硒(APS-SeNPs)。通过系统综述黄芪硒多糖的制备方法、结构特性、生物活性及构效关系,并展望其应用前景。目前制备方法主要包括生物转化法和化学合成法,硒化后产物溶解性、稳定性显著提高,并可形成粒径均匀的纳米颗粒,生物利用度明显提升。研究表明,黄芪硒多糖表现出优于APS的抗氧化、免疫调节、抗肿瘤、保肝等药理活性,且APS-SeNPs可作为良好药物载体与其他活性成分协同增效。构效关系表明其活性与硒含量、相对分子质量及纳米结构密切相关。目前该领域仍面临硒化位点解析不足、系统毒理学研究缺乏等挑战,后续应加强制备工艺优化、安全性评价及临床转化研究,推动其在医药和功能食品领域的应用与发展。
[Key word]
[Abstract]
Astragalus polysaccharides (APS) are the principal bioactive constituents of Huangqi (Astragali Radix), exhibiting diverse pharmacological activities. However, their clinical application is limited by challenges including high molecular weight, low solubility, and consequently poor bioavailability. Selenization modification has emerged as an effective strategy to improve the physicochemical properties and biological functions of APS, leading to the formation of selenized APS (Se-APS) and APS-selenium nanoparticles (APS-SeNPs). This review systematically summarizes the preparation methods, structural characteristics, biological activities, and structure-activity relationships of selenium-containing APS derivatives, and discusses their application prospects. Primary preparation techniques include biological transformation and chemical synthesis approaches. Following selenization, the resulting products demonstrate significantly improved solubility, stability, and bioavailability, and can form uniformly sized nanoparticles. Research indicates that selenium-containing APS derivatives exhibit superior pharmacological efficacy compared to native APS, including enhanced antioxidant, immunomodulatory, antitumor, and hepatoprotective activities. Furthermore, APS-SeNPs can serve as effective drug delivery carriers and show synergistic effects when combined with other bioactive compounds. Structure-activity relationship studies suggest that their bioactivity is closely associated with selenium content, molecular weight, and nanostructural attributes. Nevertheless, several challenges remain in this field, such as insufficient characterization of selenization sites and a lack of systematic toxicological evaluation. Future research should focus on optimizing preparation processes, strengthening safety assessments, and promoting clinical translation to advance their applications in the pharmaceutical and functional food industries.
[中图分类号]
R28
[基金项目]
甘肃省教育厅高校教师创新基金项目(2024A-321);甘肃省高等学校创新基金项目(2021A-320);甘肃卫生职业学院2024年校级课题(202407);甘肃省中药制药工艺工程研究中心开放课题(ZYGY202005)