Fang Mengqi, Zhou Yuan, He Keren, Lu Yangyuxiao, Tao Fangfang, Huang Hong
The First Affiliated Hospital of Zhejiang Chinese Medical University (Zhejiang Provincial Hospital of Chinese Medicine), Hangzhou, China.
School of Basic Medical Sciences, Zhejiang Chinese Medical University, Hangzhou, China.
Mol Neurobiol. 2025 Feb 22. doi: 10.1007/s12035-025-04775-y.
As intrinsic immune cells in the central nervous system, microglia play a crucial role in maintaining brain homeostasis. Microglia can transition from homeostasis to various responsive states in reaction to different external stimuli, undergoing corresponding alterations in glucose metabolism. In neurodegenerative diseases including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), and multiple sclerosis (MS), microglial glucose metabolic reprogramming is widespread. This reprogramming leads to changes in microglial function, exacerbating neuroinflammation and the accumulation of pathological products, thereby driving the progression of neurodegeneration. This review summarizes the specific alterations in glucose metabolism within microglia in AD, PD, ALS, and MS, as well as the corresponding treatments aimed at reprogramming glucose metabolism. Compounds that inhibit key glycolytic enzymes like hexokinase 2 (HK2) and pyruvate kinase M2 (PKM2), or activate regulators of energy metabolism such as AMP-activated protein kinase (AMPK), have shown significant potential in the treatment of various neurodegenerative diseases. However, current research faces numerous challenges, including side effects and blood-brain barrier (BBB) penetration of compounds. Screening relevant drugs from natural products, especially flavonoids, is a reliable approach. On the one hand, longtime herbal medical practices provide a certain degree of assurance regarding clinical safety, and their chemical properties contribute to effective BBB permeability. On the other hand, the concurrent anti-tumor and anti-neuroinflammatory activities of flavonoids suggest that regulation of glucose metabolism reprogramming might be a potential common mechanism of action. Notably, considering the dynamic nature of microglial metabolism, there is an urgent need to develop technologies for real-time monitoring of glucose metabolism processes, which would significantly advance research in this field.
作为中枢神经系统中的固有免疫细胞,小胶质细胞在维持大脑内环境稳态中发挥着关键作用。小胶质细胞可因不同的外部刺激而从稳态转变为各种反应状态,同时其葡萄糖代谢也会发生相应改变。在包括阿尔茨海默病(AD)、帕金森病(PD)、肌萎缩侧索硬化症(ALS)和多发性硬化症(MS)在内的神经退行性疾病中,小胶质细胞的葡萄糖代谢重编程广泛存在。这种重编程导致小胶质细胞功能发生变化,加剧神经炎症和病理产物的积累,从而推动神经退行性变的进展。本综述总结了AD、PD、ALS和MS中小胶质细胞葡萄糖代谢的具体变化,以及针对葡萄糖代谢重编程的相应治疗方法。抑制己糖激酶2(HK2)和丙酮酸激酶M2(PKM2)等关键糖酵解酶,或激活能量代谢调节因子如AMP激活蛋白激酶(AMPK)的化合物,在治疗各种神经退行性疾病方面显示出巨大潜力。然而,目前的研究面临诸多挑战,包括化合物的副作用和血脑屏障(BBB)穿透问题。从天然产物,尤其是黄酮类化合物中筛选相关药物是一种可靠的方法。一方面,长期的草药医学实践为临床安全性提供了一定程度的保障,其化学性质有助于有效穿透血脑屏障。另一方面,黄酮类化合物同时具有的抗肿瘤和抗神经炎症活性表明,调节葡萄糖代谢重编程可能是一种潜在的共同作用机制。值得注意的是,考虑到小胶质细胞代谢的动态性质,迫切需要开发实时监测葡萄糖代谢过程的技术,这将显著推动该领域的研究进展。