Han Qiusen, Wang Xinhuan, Cai Shuangfei, Liu Xueliang, Zhang Yufei, Yang Lin, Wang Chen, Yang Rong
Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, CAS Center for Excellence of Nanoscience, National Center for Nanoscience and Technology, University of Chinese Academy of Sciences, Beijing, 100190, P. R. China.
J Mater Chem B. 2018 Mar 7;6(9):1387-1393. doi: 10.1039/c7tb03053c. Epub 2018 Feb 19.
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 Aβ42 assembly and they showed multifunctional effects: inhibiting Aβ aggregation, destabilizing Aβ fibrils, decreasing Aβ-induced oxidative stress and Aβ-mediated cytotoxicity. Thus, Que NPs with enhanced bioavailability may act as a multifunctional therapeutic agent toward amyloid-related diseases.
槲皮素（Que）作为最有效的黄酮类化合物之一，因其众多的药理和生物学功能，在抗纤维化、抗氧化及其他治疗研究中受到了广泛关注。然而，其在水中溶解度低、渗透性差以及在生理介质中不稳定，限制了它在制药领域的广泛应用。在此，通过脉冲激光烧蚀（PLA）开发了一种制备槲皮素纳米颗粒（NPs）的简便方法。槲皮素纳米颗粒呈现出均匀的形态，平均直径为50 nm，分布狭窄，这表明其溶解度和药物释放活性有所增强。由于纳米颗粒在调节淀粉样蛋白纤维化过程以及抗氧化能力方面的进展，槲皮素纳米颗粒被应用于调节Aβ42组装，并显示出多功能作用：抑制Aβ聚集、使Aβ纤维不稳定、降低Aβ诱导的氧化应激和Aβ介导的细胞毒性。因此，具有更高生物利用度的槲皮素纳米颗粒可能成为治疗淀粉样蛋白相关疾病的多功能治疗剂。
