Catto Francesca, Kirschenbaum Daniel, Economides Athena E, Reuss Anna Maria, Trevisan Chiara, Caredio Davide, Dadgar-Kiani Ehsan, Mirzet Delic, Frick Lukas, Weber-Stadlbauer Ulrike, Litvinov Sergey, Koumoutsakos Petros, Lee Jin Hyung, Aguzzi Adriano
Institute of Neuropathology, University Hospital Zurich, University of Zurich, Zurich, Switzerland.
IMAI MedTech GmbH, Zurich, Switzerland.
PLoS One. 2025 May 6;20(5):e0309489. doi: 10.1371/journal.pone.0309489. eCollection 2025.
A hallmark of Alzheimer's disease (AD) is the extracellular aggregation of toxic amyloid-beta (Aβ) peptides in form of plaques. Here, we identify netoglitazone, an antidiabetic compound previously tested in humans, as an Aβ aggregation antagonist. Netoglitazone improved cognition and reduced microglia activity in a mouse model of AD. Using quantitative whole-brain three-dimensional histology (Q3D), we precisely identified brain regions where netoglitazone reduced the number and size of Aβ plaques. We demonstrate the utility of Q3D in preclinical drug evaluation for AD by providing a high-resolution brain-wide view of drug efficacy. Applying Q3D has the potential to improve pre-clinical drug evaluation by providing information that can help identify mechanisms leading to brain region-specific drug efficacy.
阿尔茨海默病(AD)的一个标志是有毒的β-淀粉样蛋白(Aβ)肽以斑块形式在细胞外聚集。在此,我们确定了奈托格列酮,一种先前已在人体进行测试的抗糖尿病化合物,它是一种Aβ聚集拮抗剂。在AD小鼠模型中,奈托格列酮改善了认知并降低了小胶质细胞活性。使用定量全脑三维组织学(Q3D),我们精确确定了奈托格列酮减少Aβ斑块数量和大小的脑区。我们通过提供药物疗效的高分辨率全脑视图,证明了Q3D在AD临床前药物评估中的效用。应用Q3D有潜力通过提供有助于确定导致脑区特异性药物疗效的机制的信息来改善临床前药物评估。