Department of Neurological Sciences, Rush University Medical Center, Chicago, IL 60612, USA.
Division of Research and Development, Jesse Brown Veterans Affairs Medical Center, Chicago, IL 60612, USA.
Sci Signal. 2021 Oct 26;14(706):eabg4747. doi: 10.1126/scisignal.abg4747.
Astrocytes are a type of glial cell that are activated in the brain tissue of patients with Alzheimer’s disease to induce the accumulation of amyloid (Aβ). We previously found that a combination of low-dose gemfibrozil (GFB; a drug approved to treat high cholesterol) and retinoic acid (RA; a vitamin A derivative) induces lysosomal bio-genesis through peroxisome proliferator–activated receptor α (PPARα)–mediated transcription of the gene encoding transcription factor EB (TFEB), a master regulator of lysosomal biogenesis and autophagy. Here, we found that the same combination (GFB-RA) enhanced the uptake of Aβ from the extracellular space and its subsequent degradation in astrocytes through a PPARα-dependent pathway. GFB-RA stimulated the abundance of both low-density lipoprotein receptor (LDLR) and TFEB in astrocytes through PPARα. LDLR was critical for Aβ uptake, whereas TFEB was critical for its degradation. GFB-RA treatment also increased autophagic flux and lysosomal activity in astrocytes. Consistent with these effects and in a manner dependent on astroglial PPARα, oral administration of GFB-RA switched astroglial activation to a neuroprotective state, lowered Aβ burden in the brain, and improved spatial learning and memory in the 5XFAD mouse model of Alzheimer’s disease. These findings uncover a new function of PPARα in stimulating astroglial uptake and degradation of Aβ and suggest possible repurposing of GFB-RA combination therapy for AD.
星形胶质细胞是一种神经胶质细胞,在阿尔茨海默病患者的脑组织中被激活,以诱导淀粉样蛋白 (Aβ) 的积累。我们之前发现,小剂量吉非贝齐 (GFB; 一种用于治疗高胆固醇的药物) 和维甲酸 (RA; 维生素 A 的衍生物) 的组合通过过氧化物酶体增殖物激活受体 α (PPARα) 介导转录编码转录因子 EB (TFEB) 的基因诱导溶酶体生物发生,TFEB 是溶酶体生物发生和自噬的主要调节因子。在这里,我们发现相同的组合 (GFB-RA) 通过 PPARα 依赖性途径增强了星形胶质细胞从细胞外空间摄取 Aβ 及其随后的降解。GFB-RA 通过 PPARα 刺激星形胶质细胞中低密度脂蛋白受体 (LDLR) 和 TFEB 的丰度。LDLR 对于 Aβ 的摄取至关重要,而 TFEB 对于其降解至关重要。GFB-RA 处理还增加了星形胶质细胞中的自噬流和溶酶体活性。与这些作用一致,并且以依赖星形胶质细胞 PPARα 的方式,GFB-RA 的口服给药将星形胶质细胞的激活转变为神经保护状态,降低了大脑中的 Aβ 负担,并改善了阿尔茨海默病 5XFAD 小鼠模型的空间学习和记忆。这些发现揭示了 PPARα 在刺激星形胶质细胞摄取和降解 Aβ 中的新功能,并表明 GFB-RA 联合治疗可能用于 AD 的重新定位。