Departament of Biochemistry and Physiology, Physiology Section, Faculty of Pharmacy and Food Science, Universitat de Barcelona, Av. Joan XXIII 27/31, 08028 Barcelona, Spain.
Laboratory of Cellular and Molecular Pathology, Instituto de Ciencias Biomédicas, Facultad de Ciencias de la Salud, Universidad Autónoma de Chile, Talca 3460000, Chile.
Int J Mol Sci. 2023 Sep 16;24(18):14177. doi: 10.3390/ijms241814177.
Licochalcone A (Lico-A) is a flavonoid compound derived from the root of the Glycyrrhiza species, a plant commonly used in traditional Chinese medicine. While the Glycyrrhiza species has shown promise in treating various diseases such as cancer, obesity, and skin diseases due to its active compounds, the investigation of Licochalcone A's effects on the central nervous system and its potential application in Alzheimer's disease (AD) treatment have garnered significant interest. Studies have reported the neuroprotective effects of Lico-A, suggesting its potential as a multitarget compound. Lico-A acts as a PTP1B inhibitor, enhancing cognitive activity through the BDNF-TrkB pathway and exhibiting inhibitory effects on microglia activation, which enables mitigation of neuroinflammation. Moreover, Lico-A inhibits c-Jun N-terminal kinase 1, a key enzyme involved in tau phosphorylation, and modulates the brain insulin receptor, which plays a role in cognitive processes. Lico-A also acts as an acetylcholinesterase inhibitor, leading to increased levels of the neurotransmitter acetylcholine (Ach) in the brain. This mechanism enhances cognitive capacity in individuals with AD. Finally, Lico-A has shown the ability to reduce amyloid plaques, a hallmark of AD, and exhibits antioxidant properties by activating the nuclear factor erythroid 2-related factor 2 (Nrf2), a key regulator of antioxidant defense mechanisms. In the present review, we discuss the available findings analyzing the potential of Lico-A as a neuroprotective agent. Continued research on Lico-A holds promise for the development of novel treatments for cognitive disorders and neurodegenerative diseases, including AD. Further investigations into its multitarget action and elucidation of underlying mechanisms will contribute to our understanding of its therapeutic potential.
甘草查尔酮 A(Lico-A)是一种黄酮类化合物,来源于甘草属植物的根,这种植物常用于中药。由于甘草属植物中的活性化合物,它在治疗各种疾病方面显示出了前景,如癌症、肥胖和皮肤病。然而,甘草查尔酮 A 对中枢神经系统的影响及其在阿尔茨海默病(AD)治疗中的潜在应用的研究引起了广泛关注。研究报告了 Lico-A 的神经保护作用,表明其可能是一种多靶点化合物。Lico-A 作为 PTP1B 抑制剂,通过 BDNF-TrkB 途径增强认知活性,并对小胶质细胞激活表现出抑制作用,从而减轻神经炎症。此外,Lico-A 抑制 c-Jun N 末端激酶 1,这是一种参与 tau 磷酸化的关键酶,并调节脑胰岛素受体,这在认知过程中起着重要作用。Lico-A 还作为乙酰胆碱酯酶抑制剂,导致大脑中神经递质乙酰胆碱(Ach)水平升高。这种机制增强了 AD 患者的认知能力。最后,Lico-A 显示出减少淀粉样斑块的能力,淀粉样斑块是 AD 的一个标志,并通过激活核因子红细胞 2 相关因子 2(Nrf2)发挥抗氧化作用,Nrf2 是抗氧化防御机制的关键调节剂。在本综述中,我们讨论了分析 Lico-A 作为神经保护剂的潜力的现有发现。对 Lico-A 的进一步研究有望为认知障碍和神经退行性疾病(包括 AD)的新型治疗方法的发展提供新的机会。对其多靶点作用和潜在机制的进一步研究将有助于我们理解其治疗潜力。