Dai Kunkun, Wu Jiayi, Liu Xinyang, Wang Suilou, Liu Yihang, Li Hehe, Wang Haixiang
Department of Food Nutrition and Health, School of Engineering, China Pharmaceutical University Nanjing 211198 China
Beijing Laboratory of Food Quality and Safety, Key Laboratory of Alcoholic Beverages Quality and Safety of China Light Industry, Beijing Technology and Business University Beijing 100048 China
RSC Adv. 2024 Mar 20;14(14):9472-9481. doi: 10.1039/d3ra08936c.
Quercetin (QCT) has a variety of pharmacological effects, such as antioxidant, antibacterial, anticancer, anticardiovascular and antiaging effects. However, its poor water solubility, stability and bioavailability limit its applications. The special structure of cyclodextrins and their derivatives with a hydrophobic inner cavity and hydrophilic outer wall can load a variety of hydrophobic drugs of a suitable size and shape, thereby improving the stability and solubility of these molecules. In this study, an inclusion complex of quercetin and sulfobutylether-β-cyclodextrin was prepared. It was characterized FT-IR, UV, H NMR, XRD, DSC, and SEM analysis, which revealed the successful formation of the inclusion complex. biological activity estimations were carried out and the results indicated that the inclusion complex displayed higher antioxidative and antibacterial properties compared with free QCT. In addition, the mechanisms of inclusion were explored using H NMR analysis and docking calculations, thus providing a theoretical basis for obtaining an inclusion complex.
槲皮素（QCT）具有多种药理作用，如抗氧化、抗菌、抗癌、抗心血管和抗衰老作用。然而，其较差的水溶性、稳定性和生物利用度限制了其应用。环糊精及其衍生物具有特殊结构，其内腔疏水而外壁亲水，能够负载各种尺寸和形状合适的疏水药物，从而提高这些分子的稳定性和溶解性。在本研究中，制备了槲皮素与磺丁基醚-β-环糊精的包合物。通过傅里叶变换红外光谱（FT-IR）、紫外光谱（UV）、核磁共振氢谱（H NMR）、X射线衍射（XRD）、差示扫描量热法（DSC）和扫描电子显微镜（SEM）分析对其进行了表征，结果表明成功形成了包合物。进行了生物活性评估，结果表明与游离QCT相比，包合物表现出更高的抗氧化和抗菌性能。此外，利用核磁共振氢谱分析和对接计算探索了包合机制，从而为获得包合物提供了理论依据。
