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黄酮类和查尔酮类骨架作为β-分泌酶1(BACE1)抑制剂的最新进展

Flavonoid and Chalcone Scaffolds as Inhibitors of BACE1: Recent Updates.

作者信息

Narayanan Anishma Payyappilliparambil, Jayan Jayalakshmi, Sudevan Sachithra Thazhathuveedu, Dhyani Archana, Zachariah Subin Mary, Mathew Bijo

机构信息

Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi, Kerala-682041, India.

School of Pharmacy, Graphic Era Hill University, Dehradun, 248007, Uttarakhand, India.

出版信息

Comb Chem High Throughput Screen. 2024;27(9):1243-1256. doi: 10.2174/1386207326666230731092409.

Abstract

Flavonoids and chalcones are two major classes of chemical moieties that have a vast background of pharmacological activities. Chalcone is a subclass of flavonoids whose therapeutic potential has been implicated due to an array of bioactivities. A lot of research works have shown interest in investigating the neuroprotective effect of these molecules, and have revealed them to be much more potent molecules that can be used to treat neurodegenerative disorders. Beta-site APP cleaving enzyme (BACE1), which is majorly found in the brain, is one of the reasons behind the development of Alzheimer's disease (AD). Flavonoids and chalcones have proven clinical data that they inhibit the production of Aβ plaques that are involved in the progression of AD. In this article, we have provided a detailed chronological review of the research work on the BACE1 inhibiting potency of both flavonoids and chalcones. Almost all the flavonoids and chalcones mentioned in this article have shown very good and BACE1 inhibiting activity. The docking studies and the structural importance of some BACE1-inhibiting flavonoids, as well as chalcones, are also mentioned here.

摘要

黄酮类化合物和查耳酮是两类具有广泛药理活性背景的化学基团。查耳酮是黄酮类化合物的一个亚类,因其一系列生物活性而具有潜在的治疗价值。许多研究致力于探究这些分子的神经保护作用,并发现它们是可用于治疗神经退行性疾病的更有效分子。主要存在于大脑中的β-淀粉样前体蛋白裂解酶1(BACE1)是阿尔茨海默病(AD)发病的原因之一。黄酮类化合物和查耳酮已有临床数据证明它们能抑制与AD进展相关的Aβ斑块的产生。在本文中,我们按时间顺序详细综述了关于黄酮类化合物和查耳酮对BACE1抑制效力的研究工作。本文提及的几乎所有黄酮类化合物和查耳酮都表现出了非常好的BACE1抑制活性。这里还提到了一些抑制BACE1的黄酮类化合物以及查耳酮的对接研究和结构重要性。

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