College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, 1688 Meiling Avenue, Nanchang 330004, China.
Key Laboratory of Modern Preparation of Traditional Chinese Medicines, Ministry of Education, Jiangxi University of Chinese Medicine, 1688 Meiling Avenue, Nanchang 330004, China.
Molecules. 2022 Oct 14;27(20):6893. doi: 10.3390/molecules27206893.
Alzheimer's disease is the most common neurodegenerative disease, characterized by memory loss and cognitive dysfunction. Raspberry fruits contain polyphenols which have antioxidant and anti-inflammatory properties. In this study, we used molecular imprinting technology to efficiently isolate phenolic components from the raspberry ethyl acetate extracts. Six phenolic components (ellagic acid, tiliroside, kaempferol-3-o-rutoside, gallic acid, ferulic acid and vanillic acid) were identified by UPLC-Q-TOF-MS analysis. Molecular docking was used to predict the anti-inflammatory effects and anti-Alzheimer's potential of these isolated compounds, which showed a good binding ability to diseases and related proteins. However, the binding energy and docking fraction of ellagic acid, tiliroside, and kaempferol-3-o-rutoside were better than those of gallic acid, ferulic acid and vanillic acid. Additionally, by studying the effects of these six phenolic components on the LPS-induced secretion of inflammatory mediators in murine microglial (BV2) cells, it was further demonstrated that they were all capable of inhibiting the secretion of NO, IL-6, TNF-α, and IL-1β to a certain extent. However, ellagic acid, tiliroside, and kaempferol-3-o-rutoside have better inhibitory effects compared to others. The results obtained suggest that the phenolic components extracted from ethyl acetate extracts of raspberry by molecularly imprinted polymers have the potential to inhibit the progression of Alzheimer's disease.
阿尔茨海默病是最常见的神经退行性疾病,其特征是记忆力丧失和认知功能障碍。树莓果实含有具有抗氧化和抗炎特性的多酚。在这项研究中,我们使用分子印迹技术从树莓乙酸乙酯提取物中高效分离酚类成分。通过 UPLC-Q-TOF-MS 分析鉴定了六种酚类成分(鞣花酸、三叶豆紫檀苷、山奈酚-3-O-芦丁糖苷、没食子酸、阿魏酸和香草酸)。分子对接用于预测这些分离化合物的抗炎作用和抗阿尔茨海默病潜力,结果表明它们与疾病和相关蛋白具有良好的结合能力。然而,鞣花酸、三叶豆紫檀苷和山奈酚-3-O-芦丁糖苷的结合能和对接分数优于没食子酸、阿魏酸和香草酸。此外,通过研究这六种酚类成分对 LPS 诱导的小鼠小胶质细胞(BV2)细胞中炎症介质分泌的影响,进一步证明它们都能在一定程度上抑制 NO、IL-6、TNF-α和 IL-1β的分泌。然而,鞣花酸、三叶豆紫檀苷和山奈酚-3-O-芦丁糖苷的抑制作用优于其他三种。研究结果表明,通过分子印迹聚合物从树莓乙酸乙酯提取物中提取的酚类成分具有抑制阿尔茨海默病进展的潜力。
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