紫癜素,一种天然的蒽醌染料,在神经保护和神经系统疾病的治疗潜力。

IF 5.3 2区 医学 Q2 IMMUNOLOGY
Aya M Mustafa, Ghadir A Sayed, Shymaa Hatem, Roxane Abdel-Gawad Moussa, Dina M Hal, Mahmoud A Mansour, Mohamed S Abd El Hafeez
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引用次数: 0

摘要

紫癜素(1,2,4-三羟基-9,10-蒽醌)是一种天然存在的蒽醌色素,主要来源于Rubia物种。除了作为天然染料的传统用途外,紫癜蛋白最近因其多方面的药理活性而受到关注,特别是在神经保护方面。本文概述了通过莽草酸盐、甲羟戊酸盐和甲基赤藓糖醇磷酸途径形成蒽醌的生物合成途径,最终生成紫外光素。结构-活性关系分析强调了羟基取代通过自由基稳定、DNA嵌入和金属螯合在调节抗氧化、抗癌、抗菌和神经保护特性方面的关键作用。来自临床前研究的证据表明,紫癜蛋白主要通过抗tau聚集、胆碱酯酶抑制、血清素能调节、抗氧化活性和抗炎机制,在阿尔茨海默病、抑郁症、缺血性中风和年龄相关的认知衰退中发挥有益作用。虽然紫癜蛋白具有较低的急性毒性和良好的药效学,但其治疗翻译仍然受到溶解度差、代谢快和脑生物利用度低的限制。人们正在探索以纳米技术为基础的配方和分子修饰来克服这些挑战。总之,紫癜蛋白是一种多功能生物活性支架,具有开发多功能神经保护剂的巨大潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Therapeutic potential of purpurin, a natural anthraquinone dye, in neuroprotection and neurological disorders.

Purpurin (1,2,4-trihydroxy-9,10-anthraquinone) is a naturally occurring anthraquinone pigment derived primarily from Rubia species. Beyond its traditional use as a natural dye, purpurin has recently gained attention for its multifaceted pharmacological activities, particularly in neuroprotection. This review outlines the biosynthetic pathways leading to anthraquinone formation via the shikimate, mevalonate, and methylerythritol phosphate routes, culminating in the generation of purpurin. Structure-activity relationship analyses highlight the critical role of hydroxyl substitutions in modulating antioxidant, anticancer, antibacterial, and neuroprotective properties through radical stabilization, DNA intercalation, and metal chelation. Evidence from preclinical studies indicates that purpurin exerts beneficial effects in Alzheimer's disease, depression, ischemic stroke, and age-related cognitive decline, primarily through anti-tau aggregation, cholinesterase inhibition, serotonergic modulation, antioxidant activity, and anti-inflammatory mechanisms. While purpurin exhibits low acute toxicity and promising pharmacodynamics, its therapeutic translation remains limited by poor solubility, rapid metabolism, and low brain bioavailability. Nanotechnology-based formulations and molecular modifications are being explored to overcome these challenges. Collectively, purpurin represents a versatile bioactive scaffold with considerable potential for the development of multifunctional neuroprotective agents.

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来源期刊
Inflammopharmacology
Inflammopharmacology IMMUNOLOGYTOXICOLOGY-TOXICOLOGY
CiteScore
8.00
自引率
3.40%
发文量
200
期刊介绍: Inflammopharmacology is the official publication of the Gastrointestinal Section of the International Union of Basic and Clinical Pharmacology (IUPHAR) and the Hungarian Experimental and Clinical Pharmacology Society (HECPS). Inflammopharmacology publishes papers on all aspects of inflammation and its pharmacological control emphasizing comparisons of (a) different inflammatory states, and (b) the actions, therapeutic efficacy and safety of drugs employed in the treatment of inflammatory conditions. The comparative aspects of the types of inflammatory conditions include gastrointestinal disease (e.g. ulcerative colitis, Crohn''s disease), parasitic diseases, toxicological manifestations of the effects of drugs and environmental agents, arthritic conditions, and inflammatory effects of injury or aging on skeletal muscle. The journal has seven main interest areas: -Drug-Disease Interactions - Conditional Pharmacology - i.e. where the condition (disease or stress state) influences the therapeutic response and side (adverse) effects from anti-inflammatory drugs. Mechanisms of drug-disease and drug disease interactions and the role of different stress states -Rheumatology - particular emphasis on methods of measurement of clinical response effects of new agents, adverse effects from anti-rheumatic drugs -Gastroenterology - with particular emphasis on animal and human models, mechanisms of mucosal inflammation and ulceration and effects of novel and established anti-ulcer, anti-inflammatory agents, or antiparasitic agents -Neuro-Inflammation and Pain - model systems, pharmacology of new analgesic agents and mechanisms of neuro-inflammation and pain -Novel drugs, natural products and nutraceuticals - and their effects on inflammatory processes, especially where there are indications of novel modes action compared with conventional drugs e.g. NSAIDs -Muscle-immune interactions during inflammation [...]
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