Zhang Lei Justan, Salekeen Rahagir, Soto-Palma Carolina, Elsallabi Osama, Ye Hongping, Hughes Brian, Zhang Borui, Nunes Allancer, Lee Kyooa, Xu Wandi, Mohamed Abdalla, Piepgras Ellie, McGowan Sara J, Angelini Luise, O'Kelly Ryan, Han Xianlin, Niedernhofer Laura J, Robbins Paul D
Institute on the Biology of Aging and Metabolism and the Department of Biochemistry, Molecular Biology and Biophysics, University of Minnesota, Minneapolis, MN, USA.
Department of Medicine and Aging Sciences, University "G. d'Annunzio" of Chieti-Pescara, Chieti, Italy.
bioRxiv. 2024 Oct 14:2024.10.14.618023. doi: 10.1101/2024.10.14.618023.
Cellular senescence is a key driver of the aging process and contributes to tissue dysfunction and age-related pathologies. Senolytics have emerged as a promising therapeutic intervention to extend healthspan and treat age-related diseases. Through a senescent cell-based phenotypic drug screen, we identified a class of conjugated polyunsaturated fatty acids, specifically α-eleostearic acid and its methyl ester derivative, as novel senolytics that effectively killed a broad range of senescent cells, reduced tissue senescence, and extended healthspan in mice. Importantly, these novel lipids induced senolysis through ferroptosis, rather than apoptosis or necrosis, by exploiting elevated iron, cytosolic PUFAs and ROS levels in senescent cells. Mechanistic studies and computational analyses further revealed their key targets in the ferroptosis pathway, ACSL4, LPCAT3, and ALOX15, important for lipid-induced senolysis. This new class of ferroptosis-inducing lipid senolytics provides a novel approach to slow aging and treat age-related disease, targeting senescent cells that are primed for ferroptosis.
细胞衰老乃是衰老进程的关键驱动因素,且会导致组织功能障碍及与年龄相关的病症。衰老细胞溶解剂已成为一种有望延长健康寿命并治疗与年龄相关疾病的治疗干预手段。通过基于衰老细胞的表型药物筛选,我们鉴定出一类共轭多不饱和脂肪酸,特别是α-桐酸及其甲酯衍生物,作为新型衰老细胞溶解剂,它们能有效杀死多种衰老细胞,减少组织衰老,并延长小鼠的健康寿命。重要的是,这些新型脂质通过利用衰老细胞中铁、胞质多不饱和脂肪酸和活性氧水平的升高,通过铁死亡而非凋亡或坏死来诱导衰老细胞溶解。机制研究和计算分析进一步揭示了它们在铁死亡途径中的关键靶点,即ACSL4、LPCAT3和ALOX15,这些靶点对于脂质诱导的衰老细胞溶解至关重要。这类新型诱导铁死亡的脂质衰老细胞溶解剂提供了一种新方法来延缓衰老并治疗与年龄相关的疾病,靶向那些易于发生铁死亡的衰老细胞。