Institute of Medical Science, University of Toronto, 1 King's College Circle, Toronto, ON M5S 3E1, Canada.
New World Laboratories, 275 Boul. Armand-Frappier, Laval, QC H7V 4A7, Canada.
Int J Mol Sci. 2024 Feb 1;25(3):1786. doi: 10.3390/ijms25031786.
Stroke results in neuronal cell death, which causes long-term disabilities in adults. Treatment options are limited and rely on a narrow window of opportunity. Apoptosis inhibitors demonstrate efficacy in improving neuronal cell survival in animal models of stroke. However, many inhibitors non-specifically target apoptosis pathways and high doses are needed for treatment. We explored the use of a novel caspase-3/7 inhibitor, New World Laboratories (NWL) 283, with a lower IC50 than current caspase-3/7 inhibitors. We performed in vitro and in vivo assays to determine the efficacy of NWL283 in modulating cell death in a preclinical model of stroke. In vitro and in vivo assays show that NWL283 enhances cell survival of neural precursor cells. Delivery of NWL283 following stroke enhances endogenous NPC migration and leads to increased neurogenesis in the stroke-injured cortex. Furthermore, acute NWL283 administration is neuroprotective at the stroke injury site, decreasing neuronal cell death and reducing microglia activation. Coincident with NWL283 delivery for 8 days, stroke-injured mice exhibited improved functional outcomes that persisted following cessation of the drug. Therefore, we propose that NWL283 is a promising therapeutic warranting further investigation to enhance stroke recovery.
中风会导致神经元细胞死亡,从而导致成年人长期残疾。治疗选择有限,且依赖于狭窄的治疗时机窗口。凋亡抑制剂在改善中风动物模型中的神经元细胞存活方面显示出疗效。然而,许多抑制剂非特异性地靶向凋亡途径,且需要高剂量进行治疗。我们探索了使用一种新型半胱天冬酶-3/7 抑制剂(New World Laboratories [NWL] 283),其 IC50 低于当前的半胱天冬酶-3/7 抑制剂。我们进行了体外和体内实验,以确定 NWL283 在调节中风前临床模型中的细胞死亡方面的疗效。体外和体内实验表明,NWL283 增强了神经前体细胞的存活。中风后给予 NWL283 可增强内源性 NPC 迁移,并导致中风损伤皮质中的神经发生增加。此外,急性给予 NWL283 可在中风损伤部位发挥神经保护作用,减少神经元细胞死亡和小胶质细胞激活。与 8 天的 NWL283 给药同时发生的是,中风损伤的小鼠表现出改善的功能结果,并且在停止药物后仍然存在。因此,我们提出 NWL283 是一种有前途的治疗方法,值得进一步研究以增强中风恢复。