Liu Yuan, Zhang Zhixian, Zhu Zeyu, Yang Yang, Peng Weijia, Chen Qiuhe, Mak Shinghung, Tism Karl Wahkeung, Pi Rongbiao
School of Medicine, Shenzhen Campus of Sun Yat-sen University, Shenzhen, 518107, China.
School of Pharmaceutical Sciences, Guangzhou University of Chinese Medicine, Guangzhou, China.
Mini Rev Med Chem. 2025;25(2):163-175. doi: 10.2174/0113895575330648240819112435.
Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that leads to cognitive decline and memory impairment. It is characterized by the accumulation of Amyloid-beta (Aβ) plaques, the abnormal phosphorylation of tau protein forming neurofibrillary tangles, and is often accompanied by neuroinflammation and oxidative stress, which contribute to neuronal loss and brain atrophy. At present, clinical anti-AD drugs are mostly single-target, improving the cognitive ability of AD patients, but failing to effectively slow down the progression of AD. Therefore, research on effective multi-target drugs for AD has become an urgent problem to address. The main derivatives of hydroxycinnamic acid, caffeic acid, and ferulic acid, are widely present in nature and have many pharmacological activities, such as antimicrobial, antioxidant, anti-inflammatory, neuroprotective, anti-Aβ deposition, and so on. The occurrence and development of AD are often accompanied by pathologies, such as oxidative stress, neuroinflammation, and Aβ deposition, suggesting that caffeic acid and ferulic acid can be used in the research on anti-AD drugs. Therefore, in this article, we have summarized the multi-target anti-AD derivatives based on caffeic acid and ferulic acid in recent years, and discussed the new design direction of cinnamic acid derivatives as backbone compounds. It is hoped that this review will provide some useful strategies for anti-AD drugs based on cinnamic acid derivatives.
阿尔茨海默病(AD)是一种进行性神经退行性疾病,会导致认知能力下降和记忆障碍。其特征是β-淀粉样蛋白(Aβ)斑块的积累、tau蛋白异常磷酸化形成神经原纤维缠结,并且常伴有神经炎症和氧化应激,这些因素会导致神经元丢失和脑萎缩。目前,临床抗AD药物大多为单靶点药物,虽能改善AD患者的认知能力,但未能有效减缓AD的进展。因此,研发有效的AD多靶点药物已成为亟待解决的问题。羟基肉桂酸的主要衍生物咖啡酸和阿魏酸广泛存在于自然界中,并具有多种药理活性,如抗菌、抗氧化、抗炎、神经保护、抗Aβ沉积等。AD的发生和发展常伴有氧化应激、神经炎症和Aβ沉积等病理过程,这表明咖啡酸和阿魏酸可用于抗AD药物的研究。因此,在本文中,我们总结了近年来基于咖啡酸和阿魏酸的多靶点抗AD衍生物,并讨论了以肉桂酸衍生物作为骨架化合物的新设计方向。希望这篇综述能为基于肉桂酸衍生物的抗AD药物提供一些有用的策略。