State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Bioorg Chem. 2021 Aug;113:105025. doi: 10.1016/j.bioorg.2021.105025. Epub 2021 May 26.
Neuroinflammation is emerging as a crucial reason of major neurodegenerative diseases in recent years. Increasingly evidences have supported that bioactive natural products from traditional Chinese medicines have efficiency for neuroinflammation. Forsythia suspensa, a typical medicinal herb, showed potential neuroprotective and anti-inflammatory properties in previous pharmacological studies. In our research to obtain neuroprotective and anti-inflammatory natural products, three unprecedented C6-C7'/C6-C16' linked phenylethanoidglycoside dimers (1-3), three new phenylethanoidglycosides (4-6), and six known compounds (7-12) were isolated from the fruits of Forsythia suspensa. Their structures were determined by comprehensive spectroscopic data and comparison to the literature data. All isolated compounds were evaluated their neuroprotective and anti-inflammatory activities. Compounds 1 and 10 exhibited significant neuroprotective activities with the cell viability values of 75.24 ± 8.05% and 93.65 ± 10.17%, respectively, for the serum-deprivation and rotenone induced pheochromocytoma (PC12) cell injury. Meanwhile, compound 1 exhibited excellent anti-inflammatory activity against tumor necrosis factor (TNF)-α expression in LPS induced RAW264.7 cells with the IC value of 1.30 μM. This study revealed that the bioactive phenylethanoidglycosides may attenuate neuroinflammation through their neuroprotective and anti-inflammatory activities.
神经炎症近年来已成为多种重大神经退行性疾病的重要原因。越来越多的证据表明，中药中的生物活性天然产物对神经炎症具有疗效。连翘作为一种典型的药用植物，在以前的药理学研究中表现出潜在的神经保护和抗炎特性。在我们获得神经保护和抗炎天然产物的研究中，从连翘果实中分离得到了三个前所未有的 C6-C7'/C6-C16' 连接的苯乙醇苷二聚体（1-3）、三个新的苯乙醇苷（4-6）和六个已知化合物（7-12）。通过综合光谱数据和与文献数据的比较确定了它们的结构。所有分离得到的化合物均进行了神经保护和抗炎活性评价。化合物 1 和 10 表现出显著的神经保护活性，其在血清剥夺和鱼藤酮诱导的嗜铬细胞瘤（PC12）细胞损伤中的细胞活力值分别为 75.24±8.05%和 93.65±10.17%。同时，化合物 1 对脂多糖诱导的 RAW264.7 细胞中肿瘤坏死因子（TNF）-α表达表现出优异的抗炎活性，IC 值为 1.30μM。本研究表明，生物活性苯乙醇苷可能通过其神经保护和抗炎活性来减轻神经炎症。
