JNU-UPM International Joint Laboratory on Plant Oil Processing and Safety, Department of Food Science and Engineering, Jinan University, Guangzhou 510632, China.
School of Science, Monash University Malaysia, Bandar Sunway 47500, Selangor, Malaysia.
Food Chem. 2025 Feb 1;464(Pt 1):141553. doi: 10.1016/j.foodchem.2024.141553. Epub 2024 Oct 9.
Cyclolinopeptides (CLs) have anti-inflammatory, anti-osteoporosis, and anti-tumor effects, however, low water and oil solubility greatly limit their application. Herein, CLs-loaded β-cyclodextrin (β-CD) emulsions were prepared with different oil phases. The in vitro digestibility, cellular absorption, and anti-inflammatory effects were evaluated. Camellia oil diacylglycerol (CO DAG) showed enhanced dissolving ability for CLs due to high polarity. β-CD formed inclusion complexes with DAG through hydrogen bond and the emulsions showed smaller size and higher physical stability with 50 % (w/w) oil. The in vitro digestibility of the DAG emulsion was increased and the CLs' bioavailability was 13.6-fold higher than CLs in oil. The CLs-loaded Pickering emulsion digesta exhibited a higher nitric oxides (NO) inhibition rate (58.62 %) and Caco-2 cell penetration (3.09 × 10 cm/s). Therefore, emulsion formulated with β-cyclodextrin and DAG can effectively improve the solubility and bioavailability of CLs, which has significant potential for application in functional foods and pharmaceutical industry.
环酰肽（CLs）具有抗炎、抗骨质疏松和抗肿瘤作用，但低水和油溶性极大地限制了它们的应用。本文采用不同油相制备了环酰肽-β-环糊精（β-CD）乳液。评价了其体外消化率、细胞吸收和抗炎作用。由于高极性，茶籽油二酰基甘油（CO DAG）显示出增强的 CLs 溶解能力。β-CD 通过氢键与 DAG 形成包合物，乳液在 50%（w/w）油含量下具有更小的粒径和更高的物理稳定性。DAG 乳液的体外消化率增加，CLs 的生物利用度比油相中的 CLs 高 13.6 倍。载 CLs 的Pickering 乳液消化物表现出更高的一氧化氮（NO）抑制率（58.62%）和 Caco-2 细胞穿透率（3.09×10cm/s）。因此，用β-环糊精和 DAG 配制的乳液可以有效提高 CLs 的溶解度和生物利用度，在功能性食品和制药工业中有很大的应用潜力。
