Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta University, Augusta, GA 30912, United States.
Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta University, Augusta, GA 30912, United States.
Brain Res. 2021 Feb 1;1752:147222. doi: 10.1016/j.brainres.2020.147222. Epub 2020 Dec 23.
Intracerebral hemorrhage (ICH) or hemorrhagic stroke is a major public health problem with no effective treatment. Given the emerging role of epigenetic mechanisms in the pathophysiology of ICH, we tested the hypothesis that a class 1 histone deacetylase inhibitor (HDACi), Entinostat, attenuates neurodegeneration and improves neurobehavioral outcomes after ICH. To address this, we employed a preclinical mouse model of ICH and Entinostat was administered intraperitoneally one-hour post induction of ICH. Entinostat treatment significantly reduced the number of degenerating neurons and TUNEL-positive cells after ICH in comparison to vehicle-treated controls. Moreover, Entinostat treatment significantly reduced hematoma volume, T2-weighted hemorrhagic lesion volume and improved acute neurological outcomes after ICH. Further, Entinostat significantly reduced the hemin-induced release of proinflammatory cytokines in vitro. Consistently, the expression of proinflammatory microglial/macrophage marker, CD16/32, was remarkably reduced in Entinostat treated group after ICH in comparison to control. Altogether, data implicates the potential of class 1 HDACi, Entinostat, in improving acute neurological function after ICH warranting further investigation.
脑出血(ICH)或出血性中风是一个重大的公共卫生问题,目前尚无有效的治疗方法。鉴于表观遗传机制在 ICH 病理生理学中的新兴作用,我们检验了这样一个假设,即一种 I 类组蛋白去乙酰化酶抑制剂(HDACi),恩替诺特,可减轻 ICH 后的神经退行性变并改善神经行为结局。为了解决这个问题,我们采用了 ICH 的临床前小鼠模型,在 ICH 诱导后一小时通过腹腔内给药恩替诺特。与载体处理的对照组相比,恩替诺特治疗显著减少了 ICH 后神经元变性和 TUNEL 阳性细胞的数量。此外,恩替诺特治疗显著减少了 ICH 后的血肿体积、T2 加权出血病变体积,并改善了急性神经功能结局。此外,恩替诺特显著降低了血红素诱导的促炎细胞因子的释放。一致地,与对照组相比,在 ICH 后恩替诺特治疗组中促炎小胶质细胞/巨噬细胞标志物 CD16/32 的表达显著降低。总的来说,数据表明 I 类 HDACi 恩替诺特在改善 ICH 后的急性神经功能方面具有潜力,值得进一步研究。