Bennion Douglas M, Isenberg Jacob D, Harmel Allison T, DeMars Kelly, Dang Alex N, Jones Chad H, Pignataro Megan E, Graham Justin T, Steckelings U Muscha, Alexander Jon C, Febo Marcelo, Krause Eric G, de Kloet Annette D, Candelario-Jalil Eduardo, Sumners Colin
Department of Physiology and Functional Genomics and McKnight Brain Institute, College of Medicine, University of Florida, Gainesville, Florida, United States of America.
Department of Neuroscience and McKnight Brain Institute, College of Medicine, University of Florida, Gainesville, Florida, United States of America.
PLoS One. 2017 Jul 3;12(7):e0180738. doi: 10.1371/journal.pone.0180738. eCollection 2017.
Activation of the angiotensin II type 2 receptor (AT2R) by administration of Compound 21 (C21), a selective AT2R agonist, induces neuroprotection in models of ischemic stroke in young adult animals. The mechanisms of this neuroprotective action are varied, and may include direct and indirect effects of AT2R activation. Our objectives were to assess the long-term protective effects of post-stroke C21 treatments in a clinically-relevant model of stroke in aged rats and to characterize the cellular localization of AT2Rs in the mouse brain of transgenic reporter mice following stroke. Intraperitoneal injections of C21 (0.03mg/kg) after ischemic stroke induced by transient monofilament middle cerebral artery occlusion resulted in protective effects that were sustained for up to at least 3-weeks post-stroke. These included improved neurological function across multiple assessments and a significant reduction in infarct volume as assessed by magnetic resonance imaging. We also found AT2R expression to be on neurons, not astrocytes or microglia, in normal female and male mouse brains. Stroke did not induce altered cellular localization of AT2R when assessed at 7 and 14 days post-stroke. These findings demonstrate that the neuroprotection previously characterized only during earlier time points using stroke models in young animals is sustained long-term in aged rats, implying even greater clinical relevance for the study of AT2R agonists for the acute treatment of ischemic stroke in human disease. Further, it appears that this sustained neuroprotection is likely due to a mix of both direct and indirect effects stemming from selective activation of AT2Rs on neurons or other cells besides astrocytes and microglia.
给予选择性血管紧张素II 2型受体(AT2R)激动剂化合物21(C21)可激活AT2R,从而在年轻成年动物的缺血性中风模型中诱导神经保护作用。这种神经保护作用的机制多种多样,可能包括AT2R激活的直接和间接作用。我们的目标是评估中风后C21治疗在老年大鼠临床相关中风模型中的长期保护作用,并表征中风后转基因报告小鼠的小鼠脑中AT2R的细胞定位。短暂性单丝大脑中动脉闭塞诱导缺血性中风后腹腔注射C21(0.03mg/kg)可产生保护作用,该作用在中风后至少持续3周。这些作用包括多次评估中神经功能的改善以及磁共振成像评估显示梗死体积显著减小。我们还发现,在正常雌性和雄性小鼠脑中,AT2R表达于神经元,而非星形胶质细胞或小胶质细胞。中风后7天和14天评估时,AT2R的细胞定位未发生改变。这些发现表明,先前仅在年轻动物中风模型的早期时间点所表征的神经保护作用在老年大鼠中可长期持续,这意味着AT2R激动剂用于人类疾病缺血性中风急性治疗的研究具有更大的临床相关性。此外,这种持续的神经保护作用似乎可能是由于选择性激活神经元或除星形胶质细胞和小胶质细胞之外的其他细胞上的AT2R所产生的直接和间接作用共同所致。