关键词: Amyloid Anticancer Carbon dots Neurodegeneration Proteasome

Mesh : Humans Neuroprotective Agents / pharmacology chemistry Emodin / pharmacology analogs & derivatives chemistry HeLa Cells Cell Line, Tumor Drug Stability Antineoplastic Agents / pharmacology chemistry Cell Proliferation / drug effects Drug Delivery Systems Amyloid beta-Peptides / metabolism Nanoparticles / chemistry Aloe / chemistry Proteasome Endopeptidase Complex / metabolism

来  源:   DOI:10.1038/s41598-024-67397-9   PDF(Pubmed)

Abstract:
We investigate the therapeutic potential of Aloin A and Aloin B, two natural compounds derived from Aloe vera leaves, focusing on their neuroprotective and anticancer properties. The structural differences between these two epimers suggest that they may exhibit distinct pharmacological properties. Our investigations revealed that both epimers are not stable in aqueous solution and tend to degrade rapidly, with their concentration decreasing by over 50% within approximately 12 h. These results underscore the importance of addressing issues such as the need for encapsulation into effective drug delivery systems to enhance stability. ThT fluorescence experiments showed that neither compound was able to inhibit Aβ amyloid aggregation, indicating that other mechanisms may be responsible for their neuroprotective effects. Next, an equimolar mixture of Aloin A and Aloin B demonstrated an ability to inhibit proteasome in tube tests, which is suggestive of potential anticancer properties, in accordance with antiproliferative effects observed in neuroblastoma SH-SY5Y and HeLa cell lines. Higher water stability and increased antiproliferative activity were observed by encapsulation in carbon dot nanoparticles, suggesting a promising potential for further in vivo studies.
摘要:
我们研究了芦荟素A和芦荟素B的治疗潜力,来自芦荟叶的两种天然化合物,专注于它们的神经保护和抗癌特性。这两种差向异构体之间的结构差异表明它们可能表现出不同的药理学性质。我们的调查表明,两种差向异构体在水溶液中都不稳定,并且倾向于快速降解,它们的浓度在大约12小时内降低超过50%。这些结果强调了解决诸如需要包封到有效药物递送系统中以增强稳定性的问题的重要性。荧光实验表明,两种化合物都不能抑制Aβ淀粉样蛋白的聚集,表明其他机制可能负责其神经保护作用。接下来,AloinA和AloinB的等摩尔混合物在试管试验中显示出抑制蛋白酶体的能力,这暗示了潜在的抗癌特性,根据在神经母细胞瘤SH-SY5Y和HeLa细胞系中观察到的抗增殖作用。通过封装在碳点纳米颗粒中观察到更高的水稳定性和增加的抗增殖活性,这表明了进一步体内研究的潜力。
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