Institute of Molecular Science, Shanxi University, Taiyuan, 030006, China.
School of Traditional Chinese Materia Medica, Shanxi University of Chinese Medicine, Taiyuan, 030619, China.
Neurochem Int. 2019 May;125:57-66. doi: 10.1016/j.neuint.2019.02.008. Epub 2019 Feb 13.
In the study, the neuroprotectivities of forsythiaside, a main constituent of Forsythia suspensa (Thunb.) Vahl (F. suspensa, Lianqiao in Chinese), were investigated in the hippocampal slices. Forsythiaside suppressed the overexpression of cyclooxygenase-2 (COX-2) and monoacylglycerol lipase (MAGL) proteins induced by β-amyloid (Aβ) to upregulate the levels of 2-arachidonoylglycerol (2-AG), an endogenous endocannabinoids. Then the inhibition of forsythiaside on COX-2 was deeply studied by the molecular docking. Forsythiaside prevented neuroinflammation and apoptosis from Aβ insults, and this action appeared to be mediated via cannabinoid receptor 1 (CB1R)-dependent nuclear factor-κB (NF-κB) signaling pathways. More importantly, forsythiaside functionally improved Aβ-induced learning and memory deficits, which was indicated by long term potentiation (LTP). Taken together, forsythiaside may have therapeutic potential for Alzheimer's diseases (AD) by increasing the levels of 2-AG.
在这项研究中，研究人员考察了连翘苷（连翘的主要成分）在海马切片中的神经保护作用。连翘苷抑制β-淀粉样蛋白（Aβ）诱导的环氧化酶-2（COX-2）和单酰基甘油脂肪酶（MAGL）蛋白的过表达，从而上调内源性大麻素 2-花生四烯酸甘油（2-AG）的水平。随后，通过分子对接深入研究了连翘苷对 COX-2 的抑制作用。连翘苷可防止神经炎症和细胞凋亡，这一作用似乎是通过大麻素受体 1（CB1R）依赖性核因子-κB（NF-κB）信号通路介导的。更重要的是，连翘苷可改善 Aβ诱导的学习和记忆障碍，这可通过长时程增强（LTP）来证明。总之，连翘苷通过增加 2-AG 的水平可能对阿尔茨海默病（AD）具有治疗潜力。
