School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China.
School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, China; Guangdong Engineering Research Center for Lead Compounds & Drug Discovery, Guangzhou 510006, China.
Fitoterapia. 2020 Apr;142:104523. doi: 10.1016/j.fitote.2020.104523. Epub 2020 Feb 22.
The seeds of Quercus serrata Thunb. (acorns) have been served as a healthy food in Asia. In this study, five previously undescribed triterpenoids, along with nineteen known triterpenoids were isolated from acorns. Their structures were identified on account of spectroscopic analysis and GC-MS analysis after acid hydrolysis. Meanwhile, the inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in microglia cells (BV-2) of the identified triterpenoids were evaluated. All these compounds revealed overt anti-neuroinflammatory activity expect for 7. Compounds 1, 16 and 17 had potent inhibitory effects on protein and mRNA expression of iNOS and COX-2 in LPS-induced BV-2 cells. Bioactive triterpenoids 1, 2, 16 and 17 could block LPS-induced NF-κB nuclear translocation. This study suggested that acorns could be served as natural healthy product against neuroinflammatory-associated diseases, such as Alzheimer's disease.
栓皮栎的种子（橡实）在亚洲一直被用作健康食品。在这项研究中，从橡实中分离出了五个以前未描述过的三萜类化合物，以及十九个已知的三萜类化合物。它们的结构是通过光谱分析和酸水解后的 GC-MS 分析确定的。同时，评估了鉴定出的三萜类化合物对脂多糖（LPS）诱导的小胶质细胞（BV-2）中一氧化氮（NO）产生的抑制作用。除了 7 号化合物外，所有这些化合物都表现出明显的抗神经炎症活性。化合物 1、16 和 17 对 LPS 诱导的 BV-2 细胞中 iNOS 和 COX-2 的蛋白和 mRNA 表达具有很强的抑制作用。具有生物活性的三萜类化合物 1、2、16 和 17 可以阻止 LPS 诱导的 NF-κB 核转位。这项研究表明，橡实可以作为天然健康产品，用于治疗与神经炎症相关的疾病，如阿尔茨海默病。
