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Quercetin nanoparticles with enhanced bioavailability as multifunctional agents toward amyloid induced neurotoxicity

机译:槲皮素纳米颗粒具有增强的生物利用度,作为氨基砜诱导的神经毒性的多官能剂

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摘要

Quercetin (Que), as one of the most potent flavonoids, has gained appreciable attention in anti-fibrosis, anti-oxidation and other therapeutic research due to its numerous pharmacological and biological functions. However, low aqueous solubility, poor permeability and instability in physiological media have limited its widespread application in the pharmaceutical field. Herein, a facile method for fabrication of Que nanoparticles (NPs) has been developed by pulsed laser ablation (PLA). Que NPs exhibited homogeneous morphology with an average diameter of 50 nm and narrow distributions, which revealed enhanced solubility and drug release activity. Owing to the advance of NPs in modulating the amyloid fibrillation process as well as the anti-oxidative ability, Que NPs were applied to regulate A42 assembly and they showed multifunctional effects: inhibiting A aggregation, destabilizing A fibrils, decreasing A-induced oxidative stress and A-mediated cytotoxicity. Thus, Que NPs with enhanced bioavailability may act as a multifunctional therapeutic agent toward amyloid-related diseases.
机译:槲皮素(que)作为最有效的黄酮类化合物之一,由于其许多药理学和生物学功能,抗纤维化,抗氧化和其他治疗研究中的显着关注。然而,低水溶性,生理介质中的渗透性和不稳定性有限于药物领域的广泛应用。这里,已经通过脉冲激光烧蚀(PLA)开发了一种用于制造QUE纳米颗粒(NPS)的容易方法。 QUE NPS表现出均匀的形态,平均直径为50nm和窄分布,显示出增强的溶解度和药物释放活性。由于NPS调节淀粉样蛋白原纤化过程以及抗氧化能力,QUE NPS被施用来调节A42组件,并且它们显示出多功能效应:抑制聚集,破坏纤维溶液,降低诱导的氧化应激和诱导氧化应激一种介导的细胞毒性。因此,具有增强的生物利用度的Que NP可以作为与淀粉样蛋白相关疾病的多功能治疗剂起作用。

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    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

    Univ Chinese Acad Sci Natl Ctr Nanosci &

    Technol CAS Ctr Excellence Nanosci Key Lab Biomed Effects Nanomat &

    Nanosafety Beijing 100190 Peoples R China;

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  • 正文语种 eng
  • 中图分类 分析化学;
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