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高生物利用度姜黄素:一种针对以慢性神经炎症为特征的神经退行性疾病的抗炎和神经支持性生物活性营养素。

High bioavailability curcumin: an anti-inflammatory and neurosupportive bioactive nutrient for neurodegenerative diseases characterized by chronic neuroinflammation.

作者信息

Ullah Faheem, Liang Andy, Rangel Alejandra, Gyengesi Erika, Niedermayer Garry, Münch Gerald

机构信息

Department of Pharmacology, School of Medicine, Western Sydney University, Campbelltown, NSW, Australia.

Molecular Medicine Research Group, Western Sydney University, Campbelltown, NSW, Australia.

出版信息

Arch Toxicol. 2017 Apr;91(4):1623-1634. doi: 10.1007/s00204-017-1939-4. Epub 2017 Feb 15.

Abstract

Neuroinflammation is a pathophysiological process present in a number of neurodegenerative disorders, such as Alzheimer's disease, Huntington's disease, Parkinson's disease, stroke, traumatic brain injury including chronic traumatic encephalopathy and other age-related CNS disorders. Although there is still much debate about the initial trigger for some of these neurodegenerative disorders, during the progression of disease, broad range anti-inflammatory drugs including cytokine suppressive anti-inflammatory drugs (CSAIDs) might be promising therapeutic options to limit neuroinflammation and improve the clinical outcome. One of the most promising CSAIDs is curcumin, which modulates the activity of several transcription factors (e.g., STAT, NF-κB, AP-1) and their pro-inflammatory molecular signaling pathways. However, normal curcumin preparations demonstrate low bioavailability in vivo. To increase bioavailability, preparations of high bioavailability curcumin have been introduced to achieve therapeutically relevant concentrations in target tissues. This literature review aims to summarize the pharmacokinetic and toxicity profile of different curcumin formulations.

摘要

神经炎症是许多神经退行性疾病中存在的一种病理生理过程,如阿尔茨海默病、亨廷顿舞蹈症、帕金森病、中风、包括慢性创伤性脑病在内的创伤性脑损伤以及其他与年龄相关的中枢神经系统疾病。尽管对于其中一些神经退行性疾病的初始触发因素仍存在诸多争议,但在疾病进展过程中,包括细胞因子抑制性抗炎药物(CSAIDs)在内的广泛抗炎药物可能是限制神经炎症和改善临床结果的有前景的治疗选择。最有前景的CSAIDs之一是姜黄素,它可调节多种转录因子(如STAT、NF-κB、AP-1)的活性及其促炎分子信号通路。然而,普通姜黄素制剂在体内的生物利用度较低。为提高生物利用度,已引入高生物利用度姜黄素制剂以在靶组织中达到治疗相关浓度。这篇文献综述旨在总结不同姜黄素制剂的药代动力学和毒性特征。

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