摘要
中枢神经系统(中枢神经系统)是一个重要的药物传送靶点。在黄酮类化合物对脑的可达性进行讨论时,一组来自植物的广泛已知的多种生物活性的次生代谢产物通过不同的机制实现的这一目标。最近,他们对神经系统和精神疾病的治疗理,如阿尔茨海默氏病和帕金森氏病和抑郁症,引起了广泛的关注。为了达到药物有效浓度的目标,必须跨越黄酮类化合物的血脑屏障。本文在体外和体内研究的基础上综述了低脑生物利用度的问题。除了黄酮类化合物的脂溶性,它们的渗透性将取决于膜转运蛋白的作用,尤其是那些来自于ABC超家族的的黄酮化合物。酶的元素,即β-glucuro-nidase,可以诱导降解过程和瞬态影响透气性。新颖的药物传递系统是是克服低生物利用的问题,重定从原生形式到中枢神经系统目标的可行的方法。本文对医学化学和天然产物研究的热门话题有着独特的见解。
关键词: 黄酮类化合物,脑传递,血脑屏障,通透性,转运蛋白,纳米载体,神经退行性疾病。
Current Medicinal Chemistry
Title:Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers
Volume: 23 Issue: 36
Author(s): Paula Branquinho Andrade, Clara Grosso, Patrícia Valentao, Joao Bernardo
Affiliation:
关键词: 黄酮类化合物,脑传递,血脑屏障,通透性,转运蛋白,纳米载体,神经退行性疾病。
摘要: The central nervous system (CNS) is a mythical target for drug delivery. There is an ongoing debate over the brain accessibility of flavonoids, a group of plant-derived secondary metabolites widely known by their multifarious bioactivities achieved by distinct mechanisms. Recently, their applicability in the management of neurologic and psychiatric disorders, such as Alzheimer’s and Parkinson’s diseases, and major depression, has received particular attention. To reach their target, flavonoids must cross over the ultimate obstacle - the blood-brain barrier - at pharmacologically effective concentrations. This review addresses the low brain-bioavailability issue, based on in vitro and in vivo evidences. Besides the lipophilic character of the flavonoids, their permeability will depend upon the role of membrane transporters, especially those from the ABC superfamily. The enzymatic elements, namely β-glucuro-nidase, can induce a transient deconjugation process and affect permeability, as well. Novel drug delivery systems are successful strategies to overcome the low bioavailability issue, and redirect the native forms to CNS-targets. This work bridges a solid opinion over this hot topic of medicinal chemistry and natural products research.
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Cite this article as:
Paula Branquinho Andrade, Clara Grosso, Patrícia Valentao, Joao Bernardo , Flavonoids in Neurodegeneration: Limitations and Strategies to Cross CNS Barriers, Current Medicinal Chemistry 2016; 23 (36) . https://dx.doi.org/10.2174/0929867323666160809094934
DOI https://dx.doi.org/10.2174/0929867323666160809094934 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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