Ma Xianzheng, Zhang Hui, Luan Jinkai, Tian Mingfa, Zhang Xiuxin, Sohail Ammara, Liang Dong, Liu Jiguo, Tao Fuzhan, Wang Zheng, Wang Daijie
College of Pharmacy, Food Resources Development and Health Product Creation International Joint Laboratory/Biological Engineering Technology Innovation Center of Shandong Province, Heze Branch of Qilu University of Technology, Shandong Academy of Sciences, Heze 274000, China.
Institute of Vegetables and Flowers, Chinese Academy of Agricultural Science, Beijing 100081, China.
Foods. 2025 Jun 8;14(12):2030. doi: 10.3390/foods14122030.
(1) Background: This study used a microfluidic approach to prepare paeonol (PAE) liposomes with oleanolic acid (PAE-ONLs) instead of cholesterol (PAE-CNLs), aiming to reduce cholesterol levels and enhance stability and anti-inflammatory activity. (2) Methods: The liposome formula was optimized, characterized, and tested for anti-inflammatory activities in zebrafish and RAW 264.7 macrophages, utilizing various stability and molecular interaction methods. (3) Results: The best PAE-ONL preparation conditions were 10.25 mg/mL of soy lecithin, 0.82 mg/mL of oleanolic acid, and 0.22% (wt%) of Tween 80, with an of 64.61 ± 0.42%. TEM confirmed the uniform spherical morphology, and FTIR confirmed that oleanolic acid was incorporated into the liposomes. PAE-ONLs showed better stabilities than PAE-CNLs. Molecular interaction results revealed that PAE-ONLs achieved a greater energy reduction, reaching -85.07 kJ/mol vs. the -62.64 kJ/mol of PAE-CNLs, with stable hydrogen bonding interactions. PAE-ONLs significantly reduced inflammatory cell migration in zebrafish and decreased NO, TNF-α, IL-6, and IL-1β levels in LPS-induced RAW 264.7 macrophages at 20 μg/mL. A network pharmacology analysis showed that oleanolic acid and paeonol interacted with 45 and 11 anti-inflammatory targets, respectively, and their combination in PAE-ONLs enhanced their anti-inflammatory coverage. (4) Conclusions: PAE-ONLs, utilizing oleanolic acid as a cholesterol substitute, exhibit enhanced stability and superior anti-inflammatory effects.
(1) 背景：本研究采用微流控方法制备了用齐墩果酸替代胆固醇的丹皮酚脂质体（PAE-ONLs），而非含胆固醇的丹皮酚脂质体（PAE-CNLs），旨在降低胆固醇水平并增强稳定性和抗炎活性。(2) 方法：利用各种稳定性和分子相互作用方法，对脂质体配方进行优化、表征，并在斑马鱼和RAW 264.7巨噬细胞中测试其抗炎活性。(3) 结果：最佳的PAE-ONL制备条件为10.25 mg/mL大豆卵磷脂、0.82 mg/mL齐墩果酸和0.22%（重量）吐温80，包封率为64.61±0.42%。透射电子显微镜（TEM）证实其形态为均匀球形，傅里叶变换红外光谱（FTIR）证实齐墩果酸已掺入脂质体中。PAE-ONLs比PAE-CNLs表现出更好的稳定性。分子相互作用结果表明，PAE-ONLs实现了更大的能量降低，达到-85.07 kJ/mol，而PAE-CNLs为-62.64 kJ/mol，具有稳定的氢键相互作用。PAE-ONLs在20 μg/mL时显著减少斑马鱼中的炎性细胞迁移，并降低脂多糖诱导的RAW 264.7巨噬细胞中一氧化氮（NO）、肿瘤坏死因子-α（TNF-α）、白细胞介素-6（IL-6）和白细胞介素-1β（IL-1β）的水平。网络药理学分析表明，齐墩果酸和丹皮酚分别与45个和11个抗炎靶点相互作用，它们在PAE-ONLs中的组合增强了抗炎覆盖范围。(4) 结论：以齐墩果酸作为胆固醇替代物的PAE-ONLs表现出增强的稳定性和卓越的抗炎效果。
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