Pharmacognosy Department, Faculty of Pharmacy, The British University in Egypt, Cairo, 11837, Egypt.
Pharmacognosy Department, Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt.
BMC Complement Med Ther. 2024 Jun 14;24(1):232. doi: 10.1186/s12906-024-04520-3.
Alzheimer's disease is a neurodegenerative age-related disease that primarily affects the elderly population leading to progressive memory impairments and neural deficits. It is counted as a major cause of geriatric dependency and disability. The pathogenesis of Alzheimer's disease incidence is complex and involves various hypotheses, including the cholinergic hypothesis, deposition of β-amyloid plaques, neuroinflammation, oxidative stress, and apoptosis. Conventional treatments such as donepezil aim to delay the symptoms but do not affect the progression of the disease and may cause serious side effects like hepatoxicity. The use of natural candidates for Alzheimer's disease treatment has drawn the attention of many researchers as it offers a multitargeted approach.
This current study investigates the metabolic profiles of total defatted methanolic extract of Vitex pubescens bark and its polar fractions, viz. ethyl acetate and n-butanol, using ultra-performance liquid chromatography-electrospray ionization-quadrupole time-of-flight tandem mass spectrometry(UPLC-ESI-QTOF/MS/MS) technique as well as evaluate the antioxidant using free radical scavenging assays, viz. DPPH and ABTS assays and in-vitro acetylcholinesterase inhibitory activities using Ellman's microplate assay.
Metabolic profiling revealed a total of 71, 43, and 55 metabolites tentatively identified in the defatted methanolic extract, ethyl acetate, and n-butanol fractions, respectively. Phenolic acids were the most abundant class, viz. benzoic acids, and acyl quinic acid derivatives followed by flavonoids exemplified mainly by luteolin-C-glycosides and apigenin-C-glycosides. Quantification of the total phenolic and flavonoid contents in the total defatted methanolic extract confirmed its enrichment with phenolics and flavonoids equivalent to 138.61 ± 9.39 µg gallic acid/mg extract and 119.63 ± 4.62 µg rutin/mg extract, respectively. Moreover, the total defatted methanolic extract exhibited promising antioxidant activity confirmed through DPPH and ABTS assays with a 50% inhibitory concentration (IC) value equivalent to 52.79 ± 2.16 µg/mL and 10.02 ± µg/mL, respectively. The inhibitory activity of acetylcholine esterase (AchE) was assessed using in-vitro Ellman's colorimetric assay, the total defatted methanolic extract, ethyl acetate, and n-butanol fractions exhibited IC values of 52.9, 15.1 and 108.8 µg/mL that they proved the significant inhibition of AchE activity.
The results obtained herein unraveled the potential use of the total methanolic extract of Vitex pubescens bark and its polar fractions as natural candidates for controlling Alzheimer's disease progression.
阿尔茨海默病是一种神经退行性的与年龄相关的疾病，主要影响老年人群，导致进行性记忆障碍和神经功能缺损。它被认为是导致老年依赖和残疾的主要原因之一。阿尔茨海默病发病机制复杂，涉及多种假说，包括胆碱能假说、β-淀粉样斑块沉积、神经炎症、氧化应激和细胞凋亡。传统的治疗方法，如多奈哌齐，旨在延缓症状，但不能影响疾病的进展，并且可能导致严重的副作用，如肝毒性。因此，使用天然化合物治疗阿尔茨海默病引起了许多研究人员的关注，因为它提供了一种多靶点的方法。
本研究采用超高效液相色谱-电喷雾电离-四极杆飞行时间串联质谱联用技术（UPLC-ESI-QTOF/MS/MS）分析了荆条总脱脂甲醇提取物及其极性部位（乙酸乙酯和正丁醇）的代谢谱，并采用 DPPH 和 ABTS 自由基清除实验评估其抗氧化活性，采用 Ellman 微量板法测定其体外乙酰胆碱酯酶抑制活性。
代谢谱分析共鉴定出总脱脂甲醇提取物、乙酸乙酯和正丁醇部位中分别有 71、43 和 55 种代谢产物。酚酸是最丰富的一类，包括苯甲酸和酰基奎宁酸衍生物，其次是类黄酮，主要为木樨草素-C-糖苷和芹菜素-C-糖苷。总脱脂甲醇提取物中总酚和总黄酮含量的定量分析证实其富含酚类和类黄酮，相当于 138.61 ± 9.39μg 没食子酸/毫克提取物和 119.63 ± 4.62μg 芦丁/毫克提取物。此外，总脱脂甲醇提取物表现出良好的抗氧化活性，通过 DPPH 和 ABTS 实验证实，其 50%抑制浓度（IC）值分别相当于 52.79 ± 2.16μg/mL 和 10.02 ± μg/mL。采用体外 Ellman 比色法测定乙酰胆碱酯酶（AchE）抑制活性，总脱脂甲醇提取物、乙酸乙酯和正丁醇部位的 IC 值分别为 52.9、15.1 和 108.8μg/mL，证明它们对 AchE 活性有显著抑制作用。
本研究结果揭示了荆条总甲醇提取物及其极性部位作为控制阿尔茨海默病进展的天然候选药物的潜在用途。
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