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揭示柯氏长蠕孢菌株 KU1 提取物的抗乙酰胆碱酯酶活性,作为可持续的 AChE 活性位点抑制剂。

Divulging the anti-acetylcholinesterase activity of Colletotrichum lentis strain KU1 extract as sustainable AChE active site inhibitors.

机构信息

Department of Pharmaceutical Technology and Biochemistry, Faculty of Chemistry, Gdansk University of Technology, 80-233, Gdansk, Poland.

Laboratory of Bacterial Genetics, Faculty of Chemistry, Gdansk University of Technology, 80-233, Gdansk, Poland.

出版信息

Arch Microbiol. 2022 Nov 17;204(12):713. doi: 10.1007/s00203-022-03288-9.

DOI:10.1007/s00203-022-03288-9
PMID:36396887
Abstract

Alzheimer's disease (AD), also called senile dementia is a neurodegenerative disease seen commonly in the elderly and is characterised by the formation of β-amyloid plaques and neurofibrillary tangles (NFT). Though a complete understanding of the disease is lacking, recent studies showed the role of the enzyme acetylcholinesterase (AChE) in pathogenesis. Finding new lead compounds from natural sources has always been a quest for researchers. Endophytic fungi are a set of microbes that reside within plants without causing any harm. This study focuses on screening endophytes for the production of active acetylcholinesterase inhibitors. Five endophytic fungi were isolated from Catharanthus roseus and screened for AChE inhibitory activity. Three isolates were found to inhibit AChE inhibitory activity and were distinguished based on molecular and microscopic methods. The mycelial extract was taken for the bioassay-guided column chromatography and TLC was performed on the active fraction. The GC-MS and NMR analysis identified the active compounds in the extract as 9-hexadecen-1-ol and erucamide. Molecular docking studies revealed that the compounds are thermodynamically feasible and have significant glide scores. Computational studies revealed that the hydroxyl group of 9-hexadecen-1-ol forms a hydrogen bond with Ser 293 in the active site of AChE, whereas the active site interactions were predominantly hydrophobic in the case of erucamide and are reflected in AChE inhibition assays.

摘要

阿尔茨海默病(AD),又称老年痴呆症,是一种常见于老年人的神经退行性疾病,其特征是β-淀粉样斑块和神经原纤维缠结(NFT)的形成。尽管对这种疾病的认识还不完全,但最近的研究表明,酶乙酰胆碱酯酶(AChE)在发病机制中的作用。从天然来源寻找新的先导化合物一直是研究人员的追求。内生真菌是一组存在于植物内部而不会造成任何伤害的微生物。本研究侧重于筛选内生真菌以产生活性乙酰胆碱酯酶抑制剂。从长春花中分离出 5 株内生真菌,并对其乙酰胆碱酯酶抑制活性进行筛选。发现 3 株内生真菌具有抑制乙酰胆碱酯酶的活性,并通过分子和显微镜方法进行了区分。采用菌丝体提取物进行生物活性导向柱层析,并用 TLC 对活性部分进行分析。GC-MS 和 NMR 分析鉴定出提取物中的活性化合物为 9-十六碳烯-1-醇和芥酰胺。分子对接研究表明,这些化合物在热力学上是可行的,并且具有显著的滑行分数。计算研究表明,9-十六碳烯-1-醇的羟基与 AChE 活性部位的 Ser 293 形成氢键,而芥酰胺的活性部位相互作用主要是疏水的,这反映在 AChE 抑制试验中。

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