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用于增强抗炎活性的自愈性载槲皮素的透明质酸二醛共轭氨乙基-β-环糊精与壳聚糖水凝胶席夫碱反应

Self-healing quercetin loaded hyaluronic dialdehyde conjugated aminoethyl-β-cyclodextrin and chitosan hydrogel Schiff base reaction for enhanced anti-inflammatory activity.

作者信息

Sutthisawatkul Parichat, Stapornpiriyadaj Kanyalux, Mongkhon Onuma, Taengphan Weerasak, Leepasert Theerachart, Karpkird Thitinun

机构信息

Department of Chemistry, Faculty of Science, Kasetsart University Chatuchak Bangkok 10900 Thailand

Expert Center of Innovative Herbal Products, Thailand Institute of Scientific and Technological Research Khlong Luang Pathum Thani Thailand.

出版信息

RSC Adv. 2025 Aug 20;15(36):29254-29266. doi: 10.1039/d5ra03329b. eCollection 2025 Aug 18.

DOI:10.1039/d5ra03329b
PMID:40860101
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12376988/
Abstract

In this work, hydrogels composed of hyaluronic dialdehyde (HAD) and amino-beta-cyclodextrin (ACD) incorporated with quaternary ammonium chitosan (HACC) were synthesized Schiff base reaction. The composition, morphology and mechanical properties were characterized using FTIR, H-NMR, SEM and rheological testing. Hydrogels were prepared using different molecular weights of HAD. The results showed that a higher molecular weight of HAD has increased the swelling ratio up to 1715-1835% and enhanced the mechanical properties of hydrogels. Increasing the HAD content further improved stability and mechanical properties due to a higher degree of crosslinking. Quercetin (Que), was used as a hydrophobic drug to form an inclusion complex with ACD and was loaded in HAD-ACD-HACC hydrogels. Drug release, cytotoxicity and anti-inflammatory activity were investigated . The results indicated that quercetin release was higher in acidic media than in neutral solutions. Cellular assessment of quercetin loaded 100k-2 and 1M-2 hydrogels by scratch test encouraged the migration of human keratinocyte (HaCaT) cells. The anti-inflammatory activity of quercetin loaded 100k-2 hydrogel was improved compared to free quercetin against HaCaT cells. Thus, this quercetin-loaded hydrogel system offers a promising approach for controlled drug release, enhanced anti-inflammatory and wound healing activities in various biomedical applications.

摘要

在这项工作中,通过席夫碱反应合成了由透明质酸二醛(HAD)、氨基-β-环糊精(ACD)与季铵化壳聚糖(HACC)组成的水凝胶。使用傅里叶变换红外光谱(FTIR)、氢核磁共振(H-NMR)、扫描电子显微镜(SEM)和流变学测试对其组成、形态和力学性能进行了表征。使用不同分子量的HAD制备水凝胶。结果表明,较高分子量的HAD使溶胀率提高到1715 - 1835%,并增强了水凝胶的力学性能。由于更高的交联度,增加HAD含量进一步提高了稳定性和力学性能。槲皮素(Que)作为一种疏水性药物与ACD形成包合物,并负载于HAD-ACD-HACC水凝胶中。研究了药物释放、细胞毒性和抗炎活性。结果表明,槲皮素在酸性介质中的释放高于中性溶液。通过划痕试验对负载槲皮素的100k-2和1M-2水凝胶进行细胞评估,促进了人角质形成细胞(HaCaT)的迁移。与游离槲皮素相比,负载槲皮素的100k-2水凝胶对HaCaT细胞的抗炎活性有所提高。因此,这种负载槲皮素的水凝胶系统为各种生物医学应用中的药物控释、增强抗炎和伤口愈合活性提供了一种有前景的方法。

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本文引用的文献

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Quercetin ameliorates cognitive deficit, expression of amyloid precursor gene, and pro-inflammatory cytokines in an experimental models of Alzheimer's disease in Wistar rats.槲皮素可改善阿尔茨海默病 Wistar 大鼠模型的认知缺陷、淀粉样前体基因表达和促炎细胞因子。
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Quercetin attenuates inflammation in LPS-induced lung epithelial cells via the Nrf2 signaling pathway.
槲皮素通过 Nrf2 信号通路减轻 LPS 诱导的肺上皮细胞炎症。
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