Berberine has shown an outstanding antioxidant activity, however the low bioavailability limits its applications in pharmaceutical platforms. Therefore, in this paper, after fabrication of the berberine-HSA nanoparticles by desolvation method, they were well characterized by TEM, SEM, DLS, and FTIR techniques. Afterwards the interaction of HSA and the berberine was evaluated by molecular docking analysis. Finally, the antioxidant activity of the berberine-HSA nanoparticles against H₂O₂-induced oxidative stress in cultured neurons as a model of AD was evaluated by cellular assays. The results showed that the prepared berberine-HSA nanoparticles have a spherical-shaped morphology with a size of around 100 nm and zeta potential value of -31.84 mV. The solubility value of nanoparticles was calculated to be 40.27%, with a berberine loading of 19.37%, berberine entrapment efficiency of 70.34%, and nanoparticles yield of 88.91%. Also, it was shown that the berberine is not significantly released from HSA nanoparticles within 24 hours. Afterwards, molecular docking investigation revealed that berberine spontaneously interacts with HSA through electrostatic interaction. Finally, cellular assays disclosed that the pretreatment of neuronal cultures with berberine-HSA nanoparticles decreased the H₂O₂-stimulated cytotoxicity and relevant morphological changes and enhanced the CAT activity. In conclusion, it can be indicated that the nanoformulation of the berberine can be used as a promising platform for inhibition of oxidative damage-induced Alzheimer's disease (AD).

中文翻译：

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小檗碱-白蛋白纳米颗粒：作为阿尔茨海默病模型的制备、热力学研究和评估其对初级神经元细胞氧化应激的保护作用。

小檗碱具有出色的抗氧化活性，但生物利用度低限制了其在制药平台中的应用。因此，在本文中，通过去溶剂法制备小檗碱-HSA纳米颗粒后，通过TEM、SEM、DLS和FTIR技术对其进行了很好的表征。然后通过分子对接分析评估HSA和小檗碱的相互作用。最后，小檗碱-HSA纳米颗粒对作为AD模型的培养神经元中H 2 O 2 诱导的氧化应激的抗氧化活性通过细胞测定进行了评估。结果表明，制备的小檗碱-HSA纳米颗粒呈球形，粒径约为100 nm，zeta电位值为-31.84 mV。经计算纳米粒子的溶解度值为 40.27%，黄连素负载量为 19.37%，黄连素包封率为70.34%，纳米粒收率为88.91%。此外，显示小檗碱在 24 小时内没有从 HSA 纳米颗粒中显着释放。随后，分子对接研究表明，小檗碱通过静电相互作用自发地与HSA相互作用。最后，细胞试验揭示了用小檗碱-HSA纳米粒子预处理神经元培养物降低了H 2 O 2 刺激的细胞毒性和相关的形态学变化，并增强了CAT活性。总之，可以表明小檗碱的纳米制剂可用作抑制氧化损伤诱导的阿尔茨海默病（AD）的有前景的平台。结果表明，小檗碱在 24 小时内没有从 HSA 纳米颗粒中显着释放。随后，分子对接研究表明，小檗碱通过静电相互作用自发地与HSA相互作用。最后，细胞试验揭示了用小檗碱-HSA纳米粒子预处理神经元培养物降低了H 2 O 2 刺激的细胞毒性和相关的形态学变化，并增强了CAT活性。总之，可以表明小檗碱的纳米制剂可用作抑制氧化损伤诱导的阿尔茨海默病（AD）的有前景的平台。结果表明，小檗碱在 24 小时内没有从 HSA 纳米颗粒中显着释放。随后，分子对接研究表明，小檗碱通过静电相互作用自发地与HSA相互作用。最后，细胞试验揭示了用小檗碱-HSA纳米粒子预处理神经元培养物降低了H 2 O 2 刺激的细胞毒性和相关的形态学变化，并增强了CAT活性。总之，可以表明小檗碱的纳米制剂可用作抑制氧化损伤诱导的阿尔茨海默病（AD）的有前景的平台。细胞分析表明，用小檗碱-HSA 纳米颗粒预处理神经元培养物可降低 H2O2 刺激的细胞毒性和相关的形态学变化，并增强 CAT 活性。总之，可以表明小檗碱的纳米制剂可用作抑制氧化损伤诱导的阿尔茨海默病（AD）的有前景的平台。细胞分析表明，用小檗碱-HSA 纳米颗粒预处理神经元培养物可降低 H2O2 刺激的细胞毒性和相关的形态学变化，并增强 CAT 活性。总之，可以表明小檗碱的纳米制剂可用作抑制氧化损伤诱导的阿尔茨海默病（AD）的有前景的平台。