Mani Vasudevan, Arfeen Minhajul, Dhaked Devendra Kumar, Mohammed Hamdoon A, Amirthalingam Palanisamy, Elsisi Hossam A
Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Buraydah 51452, Saudi Arabia.
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Qassim University, Buraydah 51452, Saudi Arabia.
Plants (Basel). 2023 Feb 18;12(4):934. doi: 10.3390/plants12040934.
Islamic literature has indicated that daily consumption of Ajwa dates heals a variety of chronic diseases and disorders. The current research investigates the neuroprotective effect of methanolic Ajwa seed extract (MASE) on lipopolysaccharide (LPS)-induced cognitive deficits using multiple approaches. For animal studies, MASE (200 and 400 mg/kg, p.o.) was administrated for thirty consecutive days, and four doses of LPS (250 µg/kg, i.p.) were injected to induce neurotoxicity. Memory functions were evaluated using elevated plus-maze and novel object recognition tests. Acetylcholine (ACh) and neuroinflammatory markers (cyclooxygenase (COX)-2, tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-10, and transforming growth factor (TGF)-β1) were estimated in brain tissues. Studies of molecular docking and dynamics were conducted to provide insight into the molecular-level mechanisms. MASE administration resulted in a significant reversal of LPS-induced memory impairment in both maze models. Both doses of MASE elevated the ACh levels in an LPS-treated rat brain. In addition, the extract lowered COX-2 and proinflammatory cytokines (TNF-α and IL-6) while increasing anti-inflammatory cytokines (IL-10 and TGF-β1) in LPS-treated brain tissues. Molecular modeling results revealed that the compound's ellagic acid, epicatechin, catechin, kaempferol, quercetin, and apigenin have the potential to act as a dual inhibitor of acetylcholinesterase (AChE) and COX-2 and can be responsible for the improvement of both cholinergic and inflammatory conditions, while the cinnamic acid, hesperidin, hesperetin, narengin, and rutin compounds are responsible only for the improvement of cholinergic transmission. The above compounds acted by interacting with the key residues Trp84, Asp72, Gly118, Ser200, Tyr334, and His440, which are responsible for the hydrolysis of ACh in AChE, while the COX-2 is inhibited by interacting with the residues (Val349, Leu352, Tyr355, Tyr385, Ala527, Ser530, and Leu531) of the hydrophobic channel. By promoting cholinergic activity and protecting neuroinflammation in the rat brain, MASE provides neuroprotection against LPS-induced cognitive deficits. Our preliminary findings will help with further drug discovery processes related to neuroinflammation-related neurodegeneration.
伊斯兰文学表明,每日食用阿久哇枣可治愈多种慢性疾病和失调。当前的研究使用多种方法,调查了阿久哇枣甲醇提取物(MASE)对脂多糖(LPS)诱导的认知缺陷的神经保护作用。在动物研究中,连续三十天给予MASE(200和400毫克/千克,口服),并注射四剂LPS(250微克/千克,腹腔注射)以诱导神经毒性。使用高架十字迷宫和新物体识别测试评估记忆功能。在脑组织中估计乙酰胆碱(ACh)和神经炎症标志物(环氧化酶(COX)-2、肿瘤坏死因子(TNF)-α、白细胞介素(IL)-6、IL-10和转化生长因子(TGF)-β1)。进行分子对接和动力学研究以深入了解分子水平的机制。给予MASE可使两种迷宫模型中LPS诱导的记忆损伤显著逆转。两种剂量的MASE均提高了LPS处理的大鼠脑中的ACh水平。此外,该提取物降低了LPS处理的脑组织中的COX-2和促炎细胞因子(TNF-α和IL-6),同时增加了抗炎细胞因子(IL-10和TGF-β1)。分子建模结果表明,该化合物中的鞣花酸、表儿茶素、儿茶素、山奈酚、槲皮素和芹菜素有可能作为乙酰胆碱酯酶(AChE)和COX-2的双重抑制剂,并可改善胆碱能和炎症状态,而肉桂酸、橙皮苷、橙皮素、柚皮苷和芦丁化合物仅负责改善胆碱能传递。上述化合物通过与负责AChE中ACh水解的关键残基Trp84、Asp72、Gly118、Ser200、Tyr334和His440相互作用而起作用,而COX-2则通过与疏水通道的残基(Val349、Leu352、Tyr355、Tyr385、Ala527、Ser530和Leu531)相互作用而被抑制。通过促进大鼠脑中的胆碱能活性并保护神经炎症,MASE可提供针对LPS诱导的认知缺陷的神经保护作用。我们的初步研究结果将有助于与神经炎症相关的神经退行性变的进一步药物发现过程。