Comparative chemical profiling, cholinesterase inhibitions and anti-radicals properties of essential oils from Polygonum hydropiper L: a preliminary anti- Alzheimer's study.
Comparative chemical profiling, cholinesterase inhibitions and anti-radicals properties of essential oils from Polygonum hydropiper L: a preliminary anti- Alzheimer's study.
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DOI：
10.1186/s12944-015-0145-8
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发表时间：
2015-11-04
影响因子：
4.5
通讯作者：
Ahmad S
中科院分区：
文献类型：
--
作者：
Ayaz M;Junaid M;Ullah F;Sadiq A;Khan MA;Ahmad W;Shah MR;Imran M;Ahmad S
胆碱酯酶抑制剂是开发新型和基于机制的抑制剂的重要靶点，因为它们在乙酰胆碱（ACh）神经递质的分解中起作用，以治疗包括阿尔茨海默病（AD）在内的各种神经系统疾病。类似地，自由基与各种疾病如神经退行性疾病的进展有关。由于水蓼叶和花的脂溶性和易于穿过血脑屏障的潜力，本研究旨在研究水蓼叶和花的标准化精油的抗胆碱酯酶和抗氧化潜力。用Clevenger装置分离了水蓼叶（Ph.LO）和花（Ph.FO）的挥发油。油样进行了分析，通过GC-MS，以确定主要成分和属性的抗氧化剂和抗胆碱酯酶活性的具体组成部分。乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）的抑制潜力的样品测定以下Ellman的测定。使用1，1-二苯基，2-苦基肼（DPPH）、2，2-连氮双[3-乙基苯并噻唑啉]-6-磺酸（ABTS）和过氧化氢（H2 O2）自由基清除测定进行抗氧化测定。经GC-MS分析，在Ph.LO和Ph.FO中分别鉴定出141和122个化合物。在Ph.FO中主要成分为环氧乙烷（41.42%），而在Ph. LO中主要成分为十氢萘（38.29%）.在1000 μg/ml浓度下，Ph.LO和Ph.FO对AChE的抑制率分别为87.00** %和79.66 *%，IC_（50）分别为120和220 μg/ml。加兰他敏的IC 50值为15 μg/ml。在BChE抑制实验中，当浓度为1000 μg/ml时，Ph.LO和Ph.FO对BChE的抑制率分别为82.66* %（IC_（50）为130 μg/ml）和77.50**%（IC_（50）为225 μg/ml）。在DPPH自由基清除实验中，Ph.LO和Ph.FO的IC_（50）分别为20和200 μg/ml。对ABTS和H_2O_2自由基的IC_（50）分别为180 ~ 60 μg/ml和45 ~ 50 μg/ml。在目前的研究中，水辣蓼的叶和花的精油表现出剂量依赖性的抗胆碱酯酶和抗氧化活性。叶精油的抗阿尔茨海默病作用更强，可用于进一步的体外和体内抗阿尔茨海默病研究。本文的在线版本（doi：10.1186/s12944-015-0145-8）包含补充材料，可供授权用户使用。
Cholinesterase inhibition is a vital target for the development of novel and mechanism based inhibitors, owing to their role in the breakdown of acetylcholine (ACh) neurotransmitter to treat various neurological disorders including Alzheimer’s disease (AD). Similarly, free radicals are implicated in the progression of various diseases like neurodegenerative disorders. Due to lipid solubility and potential to easily cross blood brain barrier, this study was designed to investigate the anticholinesterase and antioxidant potentials of the standardized essential oils from the leaves and flowers of Polygonum hydropiper. Essential oils from the leaves (Ph.LO) and flowers (Ph.FO) of P. hdropiper were isolated using Clevenger apparatus. Oil samples were analyzed by GC-MS to identify major components and to attribute the antioxidant and anticholinesterase activity to specific components. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potentials of the samples were determined following Ellman’s assay. Antioxidant assays were performed using 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H2O2) free radical scavenging assays. In the GC-MS analysis 141 and 122 compounds were indentified in Ph.LO and Ph.FO respectively. Caryophylene oxide (41.42 %) was the major component in Ph.FO while decahydronaphthalene (38.29 %) was prominent in Ph.LO. In AChE inhibition, Ph.LO and Ph.FO exhibited 87.00** and 79.66***% inhibitions at 1000 μg/ml with IC50 of 120 and 220 μg/ml respectively. The IC50 value for galanthamine was 15 μg/ml. In BChE inhibitory assay, Ph.LO and Ph.FO caused 82.66*** (IC50 130 μg/ml) and 77.50***% (IC50 225 μg/ml) inhibitions respectively at 1000 μg/ml concentration. In DPPH free radical scavenging assay, Ph.LO and Ph.FO exhibited IC50 of 20 and 200 μg/ml respectively. The calculated IC50s were 180 & 60 μg/ml for Ph.LO, and 45 & 50 μg/ml for Ph.FO in scavenging of ABTS and H2O2 free radicals respectively. In the current study, essential oils from leaves and flowers of P. hydropiper exhibited dose dependent anticholinesterase and antioxidant activities. Leaves essential oil were more effective and can be subjected to further in-vitro and in-vivo anti-Alzheimer’s studies. The online version of this article (doi:10.1186/s12944-015-0145-8) contains supplementary material, which is available to authorized users.