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松萝酸的抗胆碱能和抗氧化活性——活性-结构洞察

Anticholinergic and antioxidant activities of usnic acid-an activity-structure insight.

作者信息

Cetin Cakmak Kader, Gülçin İlhami

机构信息

Department of Chemistry, Faculty of Sciences, Atatürk University, 25240, Erzurum, Turkey.

出版信息

Toxicol Rep. 2019 Nov 20;6:1273-1280. doi: 10.1016/j.toxrep.2019.11.003. eCollection 2019.

Abstract

Usnic acid, as active dibenzofuran derivative, isolated and characterized from some lichen species. The aim of manuscript was to evaluate antioxidant, anticholinergic and antidiabetic potentials of usnic acid as an important natural product. Antioxidant profile of usnic acid determined by eight distinguishes bioanalytical antioxidant methods including 1,1-diphenyl-2-picrylhydrazyl (DPPH·), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS ), superoxide anion radical (O ) and N,N-dimethyl-p-phenylenediamine (DMPD ) scavenging activities, cupric ion (Cu), ferric ion (Fe) and Fe-TPTZ reducing abilities and ferrous ion (Fe) chelating activity. Usnic acid was found as potent DPPH· (IC: 49.50 μg/mL), DMPD (IC: 33.00 μg/mL), O (IC: 18.68 μg/mL), and ABTS (IC: 10.41 μg/mL) scavenging effects. Also, the inhibition effects of usnic acid were tested against some metabolic enzymes including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) linked to neurodegenerative diseases. Both enzymes play important roles in cholinergic transmission by hydrolyzing the neurotransmitter acetylcholine in cholinergic synapses, central nervous system, neuromuscular junctions and autonomic ganglia. Their inhibitors were used for clinical treatment of some neurodegenerative conditions including myasthenia gravis, Alzheimer's disease, apathy, glaucoma, postural tachycardia syndrome and dementia. Furthermore, usnic acid showed the potent inhibition profiles against AChE (IC: 1.273 nM) and BChE (IC: 0.239 nM) enzymes. The results clearly showed that usnic acid is an important natural product with antioxidant and anticholinergic potentials.

摘要

松萝酸是一种从某些地衣物种中分离并鉴定出来的活性二苯并呋喃衍生物。该论文的目的是评估松萝酸作为一种重要天然产物的抗氧化、抗胆碱能和抗糖尿病潜力。松萝酸的抗氧化特性通过八种不同的生物分析抗氧化方法来测定,包括1,1-二苯基-2-苦基肼(DPPH·)、2,2'-联氮-双-(3-乙基苯并噻唑啉-6-磺酸)(ABTS )、超氧阴离子自由基(O )和N,N-二甲基对苯二胺(DMPD )清除活性、铜离子(Cu)、铁离子(Fe)和Fe-TPTZ还原能力以及亚铁离子(Fe)螯合活性。发现松萝酸具有强大的DPPH·(IC:49.50 μg/mL)、DMPD (IC:33.00 μg/mL)、O (IC:18.68 μg/mL)和ABTS (IC:10.41 μg/mL)清除效果。此外,还测试了松萝酸对一些与神经退行性疾病相关的代谢酶的抑制作用,包括乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)。这两种酶通过水解胆碱能突触、中枢神经系统、神经肌肉接头和自主神经节中的神经递质乙酰胆碱,在胆碱能传递中发挥重要作用。它们的抑制剂被用于临床治疗一些神经退行性疾病,包括重症肌无力、阿尔茨海默病、冷漠、青光眼、体位性心动过速综合征和痴呆。此外,松萝酸对AChE(IC:1.273 nM)和BChE(IC:0.239 nM)酶显示出强大的抑制作用。结果清楚地表明,松萝酸是一种具有抗氧化和抗胆碱能潜力的重要天然产物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/614d/6889762/220f6c60ef0c/gr1.jpg

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