Department of Biology, Faculty of Biology, Alexandru Ioan Cuza University of Iasi, 700506 Iasi, Romania.
Department of Biology, Faculty of Biology, Alexandru Ioan Cuza University of Iasi, 700506 Iasi, Romania; Department of Molecular Genetics, Center for Fundamental Research and Experimental Development in Translation Medicine-TRANSCEND, Regional Institute of Oncology, 700483 Iasi, Romania.
Eur J Pharmacol. 2024 Dec 5;984:177013. doi: 10.1016/j.ejphar.2024.177013. Epub 2024 Oct 6.
The increasing attention towards age-related diseases has generated significant interest in the concept of cognitive dysfunction associated with Alzheimer's disease (AD). Certain limitations are associated with the current therapies, and flavonoids have been reported to exhibit multiple biological activities and anti-AD effects in several AD models owing to their antioxidative, anti-inflammatory, and anti-amyloidogenic properties. In this study, we performed an initial in silico predictions of the pharmacokinetic properties of three flavonoids (rhoifolin, baicalein 5,6-dimethyl ether and agathisflavone). Subsequently, we evaluated the antiamnesic and antioxidant potential of flavonoids in concentrations of 1, 3, and 5 μg/L in scopolamine (100 μM)-induced amnesic zebrafish (Danio rerio) model. Zebrafish behavior was analyzed by novel tank diving test (NTT), Y-maze, and novel object recognition test (NOR). Acetylcholinesterase (AChE) activity, brain antioxidant status and the expression of bdnf, npy, egr1, nrf2α, creb1 genes, and CREB-1 protein level was measured to elucidate the underlying mechanism of action. Our flavonoids improved memory and decreased anxiety-like behavior of scopolamine-induced amnesia in zebrafish. Also, the studied flavonoids reduced AChE activity and brain oxidative stress and upregulated the gene expression, collectively contributing to neuroprotective properties. The results of our study add new perspectives on the properties of flavonoids to regulate the evolution of neurodegenerative diseases, especially AD, by modulating the expression of genes involved in the regulation of synaptic plasticity, axonal growth, and guidance, sympathetic and vagal transmission, the antioxidant response and cell proliferation and growth.
人们越来越关注与年龄相关的疾病,这使得人们对与阿尔茨海默病(AD)相关的认知功能障碍概念产生了浓厚的兴趣。由于当前的治疗方法存在一定的局限性,而黄酮类化合物由于具有抗氧化、抗炎和抗淀粉样变性的特性,已被报道在几种 AD 模型中表现出多种生物学活性和抗 AD 作用。在本研究中,我们对三种黄酮类化合物(rhoifolin、baicalein 5,6-dimethyl ether 和 agathisflavone)的药代动力学特性进行了初步的计算机预测。随后,我们评估了黄酮类化合物在浓度为 1、3 和 5μg/L 时对东莨菪碱(100μM)诱导的健忘斑马鱼(Danio rerio)模型的抗健忘和抗氧化潜力。通过新的坦克潜水试验(NTT)、Y 型迷宫和新物体识别试验(NOR)分析斑马鱼的行为。测量乙酰胆碱酯酶(AChE)活性、大脑抗氧化状态以及 bdnf、npy、egr1、nrf2α、creb1 基因和 CREB-1 蛋白水平,以阐明其作用机制。我们的黄酮类化合物改善了记忆,减少了东莨菪碱诱导的斑马鱼健忘症的焦虑样行为。此外,研究中的黄酮类化合物还降低了 AChE 活性和大脑氧化应激,并上调了基因表达,共同发挥神经保护作用。我们的研究结果为黄酮类化合物通过调节参与调节突触可塑性、轴突生长和导向、交感和迷走神经传递、抗氧化反应以及细胞增殖和生长的基因表达来调节神经退行性疾病(特别是 AD)的发展提供了新的视角。