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柚皮素和SMER28靶向溶酶体重塑并挽救SPG11和SPG15遗传性痉挛性截瘫表型。

Naringenin and SMER28 target lysosomal reformation and rescue SPG11 and SPG15 hereditary spastic paraplegia phenotypes.

作者信息

Vantaggiato Chiara, Guarato Giulia, Brivio Francesca, Panzeri Elena, Speltoni Beatrice, Gumeni Sentiljana, Orso Genny, Santorelli Filippo Maria, Bassi Maria Teresa

机构信息

Scientific Institute IRCCS E. Medea, Laboratory of Medical Genetics, Via D. L. Monza 20, Bosisio Parini, Lecco 23842, Italy.

Department of Pharmaceutical and Pharmacological Sciences, University of Padova, Largo E. Meneghetti 2, Padova, Italy.

出版信息

Pharmacol Res. 2025 Aug;218:107836. doi: 10.1016/j.phrs.2025.107836. Epub 2025 Jun 21.

Abstract

SPG11 and SPG15 are two hereditary spastic paraplegia forms characterized by autophagosome accumulation, reduced free lysosomes and defects in autophagic lysosomal reformation (ALR). We demonstrated that attempts to rescue ALR and/or lysosome biogenesis are critical strategies for SPG15 phenotype and that SMER28 improved lysosomal reformation rescuing locomotor deficit in a SPG15 Drosophila model. Here we assessed the therapeutic potential of two FDA-approved compounds, tideglusib and naringenin, that target lysosomal function and regeneration, both registered for clinical use. Their effects were compared with those of SMER28 and of miglustat, the latter tested in a phase II clinical trial in SPG11 patients, in both SPG15 and SPG11 patient's derived cells and in the corresponding Drosophila models. We demonstrated that naringenin and SMER28 restored lysosomal and autophagic parameters in SPG15 and SPG11 cells and fly models, rescued ALR and improved locomotor deficit in vivo. Both compounds induced lysosomal tubulation, downstream of mTOR, promoting lysosomal reformation. Our work indicates that lysosomal reformation is a good strategy for herditary spastic parapegia forms with impaired lysosomal function and identifies naringenin as new modulator of this process, offering further hand to planning phase II clinical trials in SPG11-SPG15 patients.

摘要

SPG11和SPG15是两种遗传性痉挛性截瘫形式,其特征为自噬体积累、游离溶酶体减少以及自噬性溶酶体重建(ALR)缺陷。我们证明,挽救ALR和/或溶酶体生物发生的尝试是针对SPG15表型的关键策略,并且SMER28改善了溶酶体重建,挽救了SPG15果蝇模型中的运动功能缺陷。在此,我们评估了两种FDA批准的化合物替德吉布和柚皮素的治疗潜力,这两种化合物均针对溶酶体功能和再生,已注册用于临床。在SPG15和SPG11患者来源的细胞以及相应的果蝇模型中,将它们的效果与SMER28以及在SPG11患者的II期临床试验中测试过的米格列醇的效果进行了比较。我们证明,柚皮素和SMER28恢复了SPG15和SPG11细胞及果蝇模型中的溶酶体和自噬参数,挽救了ALR并改善了体内运动功能缺陷。两种化合物均诱导了mTOR下游的溶酶体成管,促进了溶酶体重建。我们的工作表明,溶酶体重建是针对溶酶体功能受损的遗传性痉挛性截瘫形式的一种良好策略,并确定柚皮素是这一过程的新调节剂,为在SPG11 - SPG15患者中开展II期临床试验提供了进一步的帮助。

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