Idris Mohammed, Azmi Mohamad Nurul, Parmusivam Thaigarajan, Supratman Unang, Litaudon Marc, Awang Khalijah
Natural Products and Synthesis Organic Research Laboratory, School of Chemical Sciences, Universiti Sains Malaysia, 11800 USM Pulau Pinang, Malaysia.
Department of Chemistry, Federal University, Yusufari Road, Gashua, 671106 Yobe, Nigeria.
Trop Life Sci Res. 2024 Oct;35(3):165-183. doi: 10.21315/tlsr2024.35.3.8. Epub 2024 Oct 7.
Alzheimer's disease (AD) is a neurodegenerative condition brought on by aging and characterised by progressive decline in cognitive function and abnormalities in the central cholnergic system. -amyloid deposits, neurofibril tangle aggregation, oxidative stress or reduced level of acetylcholine are a few causes that have been linked to AD. In this study, the bioassay-guided isolation from ethyl acetate (EtOAc) extract of bark led to the isolation of nine compounds namely, 16-phenylhexadecanoic acid (), undecylbenzene (), 3,4-dihydroxybenzoic acid (), dodecanoic acid (), tetradecanoic acid (), pentadecanoic acid (), 1-tridecene (), stigmasterol () and trimyristin (). Phytochemical analysis revealed the presence of flavonoids, steroids, lignin, alkaloids, phytosterol and triterpenoids. The DPPH scavenging activity of EtOAc extract was related to the phenolic content (116.67 ± 16.98 GAE mg/g) and other non-phenolics such as lower fatty acids. Meanwhile, the DPPH scavenging activity was found to be concentration-dependent and correlated with both flavonoid and phenolic content. Furthermore, EtOAc and methanol (MeOH) extracts of bark showed significant inhibitory activity at 100 μg/mL on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), with EtOAc extract showing 77.2% and 64.1% inhibition and MeOH extract showing 37.5% and 39.2% inhibition, respectively. Additionally, the IC for BuChE and AChE of the EtOAc extract were found to be effective, with 15.41 ± 0.78 μg/mL and 7.67 ± 0.13 μg/mL, respectively. Compound exhibited dual inhibition of 40.99 ± 1.99 μM (BuChE) and 46.83 ± 2.44 μM (AChE), while compounds and showed IC values above 200 μM. This study revealed that this plant shows a significant potential as anti-cholinesterase focusing on acetylcholinesterase (AchE) and butyrylcholinesterase (BuChE). This is the first report on and their biological activity.
阿尔茨海默病（AD）是一种由衰老引起的神经退行性疾病，其特征是认知功能逐渐衰退以及中枢胆碱能系统异常。β-淀粉样蛋白沉积、神经原纤维缠结聚集、氧化应激或乙酰胆碱水平降低是一些与AD相关的病因。在本研究中，通过生物测定指导从树皮的乙酸乙酯（EtOAc）提取物中分离出九种化合物，即16-苯基十六烷酸、十一烷基苯、3,4-二羟基苯甲酸、十二烷酸、十四烷酸、十五烷酸、1-十三烯、豆甾醇和肉豆蔻酸甘油三酯。植物化学分析表明存在黄酮类、甾体类、木质素、生物碱、植物甾醇和三萜类化合物。EtOAc提取物的DPPH清除活性与酚类含量（116.67±16.98 GAE mg/g）以及其他非酚类物质如低级脂肪酸有关。同时，发现DPPH清除活性具有浓度依赖性，并且与黄酮类和酚类含量均相关。此外，树皮的EtOAc和甲醇（MeOH）提取物在100μg/mL时对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）表现出显著的抑制活性，EtOAc提取物的抑制率分别为77.2%和64.1%，MeOH提取物的抑制率分别为37.5%和39.2%。此外，发现EtOAc提取物对BuChE和AChE的IC50有效，分别为15.41±0.78μg/mL和7.67±0.13μg/mL。化合物表现出对40.99±1.99μM（BuChE）和46.83±2.44μM（AChE）的双重抑制，而化合物和的IC50值高于200μM。本研究表明该植物作为针对乙酰胆碱酯酶（AchE）和丁酰胆碱酯酶（BuChE）的抗胆碱酯酶药物具有显著潜力。这是关于及其生物活性的首次报道。
