与阿尔茨海默病治疗相关的五叶糖提取物的抗氧化、胆碱酯酶抑制特性和抗菌潜力的评价

Rezanur Rahman, T. Islam, H. M. Faruquee, S. Akhter, Md. Anwarul Haque
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引用次数: 2

摘要

在发现治疗阿尔茨海默病(AD)的更有效、更安全的药物方面,存在巨大的未满足需求。胆碱能活性降低和氧化应激已被认为是阿尔茨海默病发病的主要因素。因此,抑制胆碱酯酶和氧化是阿尔茨海默病药物开发中两个有前途的策略。本研究测定了五谷糖的抗乙酰胆碱酯酶(AChE)活性、抗丁基胆碱酯酶(BChE)活性、DPPH自由基清除能力和抗氧化性能。本研究的目的是通过测定五谷葡萄球菌抗ache、抗bche、DPPH自由基清除能力、脂质过氧化抑制能力、抗菌潜能,找出其对不同致病菌的最低抑制浓度(MIC)。本研究利用五味子叶提取物(GPEx)来评估其抗胆碱酯酶、抗氧化潜力和抗菌性能。采用改进的Ellman法定量测定其胆碱酯酶抑制性能,并通过自由基清除和脂质过氧化抑制试验评价其抗氧化能力。采用琼脂孔扩散法测定其抑菌活性和最低抑菌浓度。甲醇提取物具有显著的双乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BChE)作用。AChE和BChE的IC50值分别为325.1±0.91、42.14±3.31 μg/ml。此外,提取物还具有清除自由基和抑制脂质过氧化的作用。提取物对DPPH和羟基自由基的清除作用IC50分别为95.6±0.68、198.0±1.39和288.7±0.91 μg/ml。提取物的植物化学筛选显示存在显著的总酚和类黄酮含量。该提取物对伤寒沙门菌、铜绿假单胞菌、金黄色葡萄球菌的抑制范围为12 ~ 16 mm。测试样品反映了潜在的抗氧化和抗胆碱酯酶抑制潜力,这可能保证了其治疗AD的有效性以及良好的抗菌性能。
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Evaluation of Antioxidant, Cholinesterase Inhibitory Properties, and Antibacterial Potentials of Glycomis Pentaphylla Leaf Extract Relevant to the Treatment of Alzheimer's Disease
There is a tremendous unmet need to discover more potent and safe drugs for the treatment of Alzheimer’s disease (AD). Reduced cholinergic activity and oxidative stress have been recognized as a major contributing factor in the pathogenesis of AD. Therefore, inhibition of cholinesterase and oxidation are the two promising strategies in the development of a drug for AD. This study determined the anti-acetylcholinesterase (AChE) activity, anti-butyrylcholinesterase (BChE) activity, DPPH free radical scavenging and antioxidant properties of Glycomis pentaphylla (Rutaceae). The objective of this study is to measure G. pentaphylla anti-AChE, anti-BChE, DPPH free radical scavenging, lipid peroxidation inhibition, antibacterial potentials to find out the MIC (minimum inhibitory concentration) against different pathogenic bacteria. G. pentaphylla leaf extract (GPEx) is exploited in the presented research to estimate its anticholinesterase, antioxidant potentials, and antibacterial properties. The cholinesterase inhibitory properties was quantified by modified Ellman method, and antioxidant potentials were evaluated by the assay of radical scavenging, and inhibition of lipid peroxidation. The antibacterial activity and minimum inhibitory concentration (MIC) were determined using agar well diffusion method. The methanolic extract exhibited significant dual acetylcholinesterase (AChE) and butyryl cholinesterase (BChE) effect. The IC50 values of AChE and BChE were 325.1±0.91, and 42.14±3.31 μg/ml. Furthermore, the extract showed radical scavenging ability, and lipid peroxidation inhibitory effect. The IC50 values of the extract for DPPH and hydroxyl free radical scavenging, and lipid peroxidation inhibition assay were 95.6±0.68, 198.0±1.39, and 288.7±0.91 μg/ml, respectively. Phytochemical screening of the extract revealed the presence of significant total phenolics and flavonoids contents. Additionally, the extract showed good effect with the zone of inhibition ranging 12–16 mm in diameter against Salmonella typhi, Pseudomonas aeruginosa, Staphylococcus aureus. The tested sample reflects potential antioxidative and anticholinesterase inhibitory potentiality which may warrant its effectiveness in the treatment of AD along with good antibacterial properties.
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