Mao Jiale, Gao Tai, Wang Lingling, Lv Xing, Zhao Xu
Faculty of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang, China.
School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, China.
Nat Prod Res. 2025 Jul 17:1-5. doi: 10.1080/14786419.2025.2534681.
This study sought to improve luteolin (Lut) solubility and bioactivity luteolin phospholipid complex (Lut-PC) preparation. Lut-PC was synthesised using solvent evaporation and characterised by multiple techniques. The optimal complexation efficiency reached 95.6% ± 0.83%. SEM, FTIR, and XRD analyses indicated that Lut-PC had an amorphous structure, differing from crystalline Lut, and its formation involved specific molecular interactions. With an octanol-water partition coefficient of 1.44, Lut-PC was more readily adsorbed. dissolution showed higher cumulative release rates in various media compared to Lut and the physical mixture. In a gouty nephropathy mouse model, Lut-PC effectively reduced uric acid, offered stronger renoprotection than Lut, and had better safety than allopurinol. Thus, phospholipid complexation is a promising method for improving Lut properties, with potential pharmaceutical applications, particularly for gouty nephropathy treatment.
本研究旨在改善木犀草素(Lut)的溶解性和生物活性,制备木犀草素磷脂复合物(Lut-PC)。采用溶剂蒸发法合成Lut-PC,并通过多种技术对其进行表征。最佳络合效率达到95.6%±0.83%。扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)和X射线衍射(XRD)分析表明,Lut-PC具有非晶态结构,与结晶态的Lut不同,其形成涉及特定的分子相互作用。Lut-PC的正辛醇-水分配系数为1.44,更易于吸附。与Lut和物理混合物相比,溶解实验表明Lut-PC在各种介质中的累积释放率更高。在痛风性肾病小鼠模型中,Lut-PC有效降低尿酸,比Lut提供更强的肾脏保护作用,且比别嘌醇具有更好的安全性。因此,磷脂络合是改善Lut性质的一种有前景的方法,具有潜在的药物应用价值,特别是在痛风性肾病治疗方面。