Dallera Carlos A, Placeres-Uray Fabiola, Mastromatteo-Alberga Patrizzia, Dominguez-Torres Maria, Balleste Alyssa F, Gorthy Aditi S, Rahimzadeh Tyler S, Aliancin Isabelle, Dietrich W Dalton, de Rivero Vaccari Juan Pablo, Jacobs Irwin C, Chlipala Elizabeth A, Benton Hannah, Zeligs Michael A, Atkins Coleen M
The Miami Project to Cure Paralysis, Department of Neurological Surgery, University of Miami Miller School of Medicine, 1095 NW 14th Terrace, Miami, FL, USA.
Boulder BioScience, LLC, Boulder, CO, USA.
Neurotherapeutics. 2025 Mar;22(2):e00531. doi: 10.1016/j.neurot.2025.e00531. Epub 2025 Feb 4.
3,3'-Diindolylmethane (DIM), a naturally occurring bis-indole found in cruciferous vegetables and produced in small amounts in the normal flora of the human gut, has demonstrated neuroprotective benefits in models of CNS hypoxia and stroke. In the CNS, DIM modulates the activation of the aryl hydrocarbon receptor (AhR) and inhibits its pro-inflammatory effects. Although capable of crossing the blood brain barrier, DIM's bioavailability is limited by its low solubility. Dispersed BR4044 provides a nanoscale high-solubility DIM suspension with the potential for treating traumatic brain injury (TBI). The present study aimed to determine whether BR4044 treatment could reduce pathology and improve behavioral recovery following moderate TBI. Male Sprague Dawley rats received moderate fluid percussion injury or sham surgery followed by vehicle or BR4044 treatment in the acute recovery period. TBI BR4044 animals showed significantly reduced cortical and hippocampal edema and lower levels of serum-derived extracellular vesicles compared to TBI Vehicle animals. BR4044 treatment of TBI animals preserved sensorimotor function and associative fear memory. Cortical contusion size and neuronal loss in the parietal cortex and CA3 region of the hippocampus were also significantly reduced with BR4044 treatment. BR4044 also decreased microbleeding and nuclear AhR at the contusion site. This translational study demonstrates that BR4044 ameliorates pathology and improves neurological outcomes following TBI by reducing brain edema, lowering acute extracellular vesicle release, modulating AhR, preserving cortical and hippocampal neurons, reducing red blood cell (RBC) extravasation into the injured brain, and promoting behavioral recovery.
3,3'-二吲哚甲烷(DIM)是一种天然存在的双吲哚,存在于十字花科蔬菜中,在人体肠道正常菌群中少量产生,已在中枢神经系统缺氧和中风模型中显示出神经保护作用。在中枢神经系统中,DIM调节芳烃受体(AhR)的激活并抑制其促炎作用。尽管DIM能够穿过血脑屏障,但其生物利用度因其低溶解度而受到限制。分散的BR4044提供了一种纳米级高溶解度的DIM悬浮液,具有治疗创伤性脑损伤(TBI)的潜力。本研究旨在确定BR4044治疗是否能减轻中度TBI后的病理变化并改善行为恢复。雄性Sprague Dawley大鼠在中度液体冲击伤或假手术后,在急性恢复期接受载体或BR4044治疗。与TBI载体动物相比,TBI BR4044动物的皮质和海马水肿明显减轻,血清来源的细胞外囊泡水平降低。BR4044治疗TBI动物可保留感觉运动功能和联想恐惧记忆。BR4044治疗还显著减少了皮质挫伤大小以及海马顶叶皮质和CA3区的神经元损失。BR4044还减少了挫伤部位的微出血和核AhR。这项转化研究表明,BR4044通过减轻脑水肿、降低急性细胞外囊泡释放、调节AhR、保护皮质和海马神经元、减少红细胞(RBC)渗入受损大脑以及促进行为恢复,改善了TBI后的病理变化并改善了神经学结果。