| 王栋伟,张卫彬,宋潇玉,等.新琼寡糖脂衍生物的合成及生物活性评价[J].中国海洋药物,2026,(4):-. |
| 新琼寡糖脂衍生物的合成及生物活性评价 |
| Synthesis and Bioactivity Evaluation of Neoagaro-oligosaccharide Lipid Derivatives |
| 投稿时间：2025-04-01 修订日期：2025-05-19 |
| DOI： |
| 中文关键词: 新琼寡糖 新琼寡糖脂 抗炎活性 抗肿瘤活性 |
| English Keywords:Neoagaro-oligosaccharides Neoagaro-oligosaccharide lipids Anti-inflammatory activity Antitumor activity |
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| 中文摘要: |
| 目的 研究新琼寡糖脂衍生物的合成方法及其抗炎和抗肿瘤活性。方法 以新琼寡糖为糖基供体，利用辛胺或硬脂胺对新琼寡糖进行脂链修饰，合成新琼寡糖脂衍生物，利用高分辨率质谱和核磁共振波谱等技术手段对其进行结构表征；利用CCK-8法检测新琼寡糖及其寡糖脂衍生物的安全性和对肿瘤细胞生长的抑制作用；利用ELISA等试剂盒检测新琼寡糖及其寡糖脂衍生物对炎症因子NO、TNF-α和IL-6释放的抑制作用。结果 新琼寡糖通过还原胺化反应成功与辛胺或硬脂胺偶联，柱层析纯化后得到了4种结构不同的新琼寡糖脂衍生物，其产率在50%左右。活性研究表明，辛胺-新琼寡糖脂衍生物无细胞毒性并能显著抑制炎症因子的释放，具有良好的抗炎作用。而硬脂胺-新琼寡糖脂衍生物有细胞毒性并能抑制肿瘤细胞的增殖，100 μg·mL-1的浓度下抑制率为80%左右，具有抗肿瘤活性。这为海洋寡糖脂类衍生物的合成及其活性研究提供了参考，为开发新型海洋药物奠定基础。 |
| English Summary: |
| Objective To investigate the synthesis method and evaluate the anti-inflammatory and antitumor activities of neoagaro-oligosaccharide lipid derivatives. Methods Using neoagaro-oligosaccharides as glycosyl donors, octylamine and stearylamine were conjugated to the oligosaccharides to synthesize neoagaro-oligosaccharide lipid derivatives. The structures were characterized using MS and NMR spectroscopy. The biosafety and tumor cell growth inhibitory effects were evaluated using the CCK-8 assay. The inhibitory effects on inflammatory mediators NO, TNF-α, and IL-6 were assessed via ELISA. Results Neoagaro-oligosaccharides were modified with octylamine or stearylamine via reductive amination and four distinct neoagaro-oligosaccharide lipid derivatives were successfully synthesized with a yield of approximately 50% after column chromatography purification. Bioactivity studies revealed that octylamine-modified derivatives exhibited no cytotoxicity and significantly inhibited the release of inflammatory factors, demonstrating potent anti-inflammatory effects. In contrast, stearylamine-modified derivatives exhibited cytotoxicity and inhibited tumor cell proliferation, with an inhibition rate of approximately 80% at 100 μg·mL-1, indicating anti-tumor potential. This study provides a reference for the synthesis and bioactivity exploration of marine oligosaccharide lipid derivatives, laying a foundation for developing novel marine-derived therapeutics. |
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