Suppr超能文献

八种药用植物的抗胆碱酯酶活性:以及寻找抗阿尔茨海默病治疗药物的研究。

Anticholinesterase Activity of Eight Medicinal Plant Species: and Studies in the Search for Therapeutic Agents against Alzheimer's Disease.

作者信息

Uddin Md Josim, Russo Daniela, Rahman Md Mahbubur, Uddin Shaikh Bokhtear, Halim Mohammad A, Zidorn Christian, Milella Luigi

机构信息

Pharmazeutisches Institut, Abteilung Pharmazeutische Biologie, Christian-Albrechts-Universität Zu Kiel, Gutenbergstraße 76, Kiel 24118, Germany.

Department of Science, University of Basilicata, Viale Dell'Ateneo Lucano 10, Potenza 85100, Italy.

出版信息

Evid Based Complement Alternat Med. 2021 Jun 25;2021:9995614. doi: 10.1155/2021/9995614. eCollection 2021.

Abstract

Many Bangladeshi medicinal plants have been used to treat Alzheimer's disease and other neurodegenerative diseases. In the present study, the anticholinesterase effects of eight selected Bangladeshi medicinal plant species were investigated. Species were selected based on the traditional uses against CNS-related diseases. Extracts were prepared using a gentle cold extraction method. cholinesterase inhibitory effects were measured by Ellman's method in 96-well microplates. (Compositae) and (Menispermaceae) were found to have the highest acetylcholinesterase inhibitory (IC 150 ± 11 and 176 ± 14 g/mL, respectively) and butyrylcholinesterase inhibitory effect (IC, 297 ± 13 and 124 ± 2 g/mL, respectively). demonstrated competitive inhibition, where showed an uncompetitive inhibition mode for acetylcholinesterase. (Smilacaceae) and (Malvaceae) were also found to show moderate AChE inhibition (IC 205 ± 31 and 221 ± 2 g/mL, respectively), although no significant BChE inhibitory effect was observed for extracts from these plant species. Among others, grandiflora (Acanthaceae) and (Compositae) were found to display noticeable AChE (IC, 252 ± 22 g/mL) and BChE (IC, 314 ± 15 g/mL) inhibitory effects, respectively. Molecular docking experiment suggested that compounds 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone (BL4) and kaempferol-3---L-rhamnopyranosyl-(1⟶6)--D-glucopyranoside (BL5) from bound stably to the binding groove of the AChE and BChE by hydrogen-bond interactions, respectively. Therefore, these compounds could be candidates for cholinesterase inhibitors. The present findings demonstrated that and are interesting objects for further studies aiming at future therapeutics for Alzheimer's disease.

摘要

许多孟加拉药用植物已被用于治疗阿尔茨海默病和其他神经退行性疾病。在本研究中,对八种选定的孟加拉药用植物物种的抗胆碱酯酶作用进行了研究。根据对中枢神经系统相关疾病的传统用途选择物种。采用温和的冷提取方法制备提取物。通过埃尔曼法在96孔微孔板中测量胆碱酯酶抑制作用。发现菊科植物和防己科植物具有最高的乙酰胆碱酯酶抑制作用(IC分别为150±11和176±14μg/mL)和丁酰胆碱酯酶抑制作用(IC分别为297±13和124±2μg/mL)。表现出竞争性抑制,而对乙酰胆碱酯酶表现出非竞争性抑制模式。虽然未观察到这些植物物种提取物对丁酰胆碱酯酶有显著抑制作用,但也发现菝葜科植物和锦葵科植物表现出中度的乙酰胆碱酯酶抑制作用(IC分别为205±31和221±2μg/mL)。其中,爵床科的大花老鸦嘴和菊科植物分别表现出显著的乙酰胆碱酯酶(IC为252±22μg/mL)和丁酰胆碱酯酶(IC为314±15μg/mL)抑制作用。分子对接实验表明,来自该植物的化合物5-羟基-3,6,7,3',4'-五甲氧基黄酮(BL4)和山柰酚-3---L-鼠李吡喃糖基-(1⟶6)--D-葡萄糖吡喃糖苷(BL5)分别通过氢键相互作用稳定地结合到乙酰胆碱酯酶和丁酰胆碱酯酶的结合槽中。因此,这些化合物可能是胆碱酯酶抑制剂的候选物。目前的研究结果表明,该植物和该植物是针对阿尔茨海默病未来治疗的进一步研究的有趣对象。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe08/8260289/836621e14b9b/ECAM2021-9995614.001.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验