Chen Xue, Zhou Xing-Yue, Lan Cai, Fu Hai-Jun, Li Zhi-Chao, Chen Meng-Yi, Wen Yong-Ping, Yu Lu, Qin Da-Lian, Wu An-Guo, Wu Jian-Ming, Zhou Xiao-Gang
Sichuan Key Medical Laboratory of New Drug Discovery and Drugability Evaluation, Luzhou Key Laboratory of Activity Screening and Druggability Evaluation for Chinese Materia Medica, School of Pharmacy, Southwest Medical University, Luzhou, Sichuan 646000, State Key Laboratory of Crop Gene Exploration and Utilization in Southwest China, Sichuan Agricultural University, Luzhou, Chengdu 611130, Sichuan, China.
Central Nervous System Drug Key Laboratory of Sichuan Province, Luzhou, Sichuan, 646000, China.
Mol Neurobiol. 2025 Jul 31. doi: 10.1007/s12035-025-05242-4.
Alzheimer's disease (AD) and Parkinson's disease (PD) are characterized by pathological protein aggregation and oxidative stress, leading to progressive neurodegeneration. Enhancing autophagy, the primary intracellular pathway for clearing misfolded proteins, represents a promising therapeutic strategy. In this study, we identify Araloside A (ARA), a triterpenoid saponin derived from Aralia elata, as a potent autophagy inducer that alleviates AD- and PD-related pathology. In neuronal cell models, ARA promotes autophagosome formation, increases LC3-II and Beclin-1 levels, and decreases P62, indicating enhanced autophagic activity. Mechanistic investigations reveal that ARA directly binds to Raf, MEK, and ERK proteins and activates autophagy in a Raf/MEK/ERK-dependent manner. This activation facilitates the clearance of APP, total Tau, phosphorylated Tau, and α-synuclein, thereby reducing cytotoxicity. Furthermore, in transgenic Caenorhabditis elegans models of AD and PD, ARA treatment alleviates protein aggregation and behavioral deficits via ERK-dependent autophagy. Together, these findings identify ARA as a natural compound that enhances autophagic clearance of neurotoxic aggregates via Raf/MEK/ERK pathway activation, offering promising therapeutic insights for neurodegenerative proteinopathies.
阿尔茨海默病(AD)和帕金森病(PD)的特征是病理性蛋白质聚集和氧化应激,导致进行性神经退行性变。增强自噬作为清除错误折叠蛋白质的主要细胞内途径,是一种有前景的治疗策略。在本研究中,我们鉴定出龙牙楤木中的三萜皂苷龙牙楤木苷A(ARA)是一种有效的自噬诱导剂,可减轻与AD和PD相关的病理变化。在神经元细胞模型中,ARA促进自噬体形成,增加LC3-II和Beclin-1水平,并降低P62,表明自噬活性增强。机制研究表明,ARA直接与Raf、MEK和ERK蛋白结合,并以Raf/MEK/ERK依赖的方式激活自噬。这种激活促进了APP、总Tau、磷酸化Tau和α-突触核蛋白的清除,从而降低细胞毒性。此外,在AD和PD的转基因秀丽隐杆线虫模型中,ARA治疗通过ERK依赖的自噬减轻蛋白质聚集和行为缺陷。总之,这些发现确定ARA是一种天然化合物,通过激活Raf/MEK/ERK途径增强神经毒性聚集体的自噬清除,为神经退行性蛋白质病提供了有前景的治疗见解。