Festoff Barry W, Ameenuddin Syed, Arnold Paul M, Wong Andrea, Santacruz Karen S, Citron Bruce A
Neurobiology Research Laboratory, Heartland Veterans Health Network, Department of Veterans Affairs Medical Center, Kansas City, Missouri 64128, USA.
J Neurochem. 2006 Jun;97(5):1314-26. doi: 10.1111/j.1471-4159.2006.03799.x. Epub 2006 Apr 21.
Minocycline, a clinically used tetracycline for over 40 years, crosses the blood-brain barrier and prevents caspase up-regulation. It reduces apoptosis in mouse models of Huntington's disease and familial amyotrophic lateral sclerosis (ALS) and is in clinical trial for sporadic ALS. Because apoptosis also occurs after brain and spinal cord (SCI) injury, its prevention may be useful in improving recovery. We analyzed minocycline's neuroprotective effects over 28 days following contusion SCI and found significant functional recovery compared to tetracycline. Histology, immunocytochemistry, and image analysis indicated statistically significant tissue sparing, reduced apoptosis and microgliosis, and less activated caspase-3 and substrate cleavage. Since our original report in abstract form, others have published both positive and negative effects of minocycline in various rodent models of SCI and with various routes of administration. We have since found decreased tumor necrosis factor-alpha, as well as caspase-3 mRNA expression, as possible mechanisms of action for minocycline's ameliorative action. These results support reports that modulating apoptosis, caspases, and microglia provide promising therapeutic targets for prevention and/or limiting the degree of functional loss after CNS trauma. Minocycline, and more potent chemically synthesized tetracyclines, may find a place in the therapeutic arsenal to promote recovery early after SCI in humans.
米诺环素是一种已临床使用40多年的四环素类药物,它能穿过血脑屏障并阻止半胱天冬酶上调。在亨廷顿舞蹈病和家族性肌萎缩侧索硬化症(ALS)的小鼠模型中,它能减少细胞凋亡,目前正用于散发性ALS的临床试验。由于脑和脊髓损伤(SCI)后也会发生细胞凋亡,因此预防细胞凋亡可能有助于促进恢复。我们分析了米诺环素在挫伤性SCI后28天内的神经保护作用,发现与四环素相比,其功能恢复显著。组织学、免疫细胞化学和图像分析表明,在组织保留、细胞凋亡减少、小胶质细胞增生减少以及活化的半胱天冬酶-3和底物裂解减少方面具有统计学意义。自从我们以摘要形式发表最初的报告以来,其他人已经发表了米诺环素在各种SCI啮齿动物模型和不同给药途径中的正反两方面作用。此后,我们发现肿瘤坏死因子-α以及半胱天冬酶-3 mRNA表达降低,这可能是米诺环素改善作用的作用机制。这些结果支持了以下报道,即调节细胞凋亡、半胱天冬酶和小胶质细胞为预防和/或限制中枢神经系统创伤后功能丧失程度提供了有希望的治疗靶点。米诺环素以及更有效的化学合成四环素类药物,可能在促进人类SCI后早期恢复的治疗手段中占有一席之地。