| 蔚欢欢,杨雨,王喆,等.透明质酸-青蒿琥酯共聚物的制备表征与抗肿瘤活性研究[J].中国海洋药物,2025,44(2):1-9. |
| 透明质酸-青蒿琥酯共聚物的制备表征与抗肿瘤活性研究 |
| Preparation and characterization of Hyaluronic acid-Artesunate conjugates and study on antitumor activity |
| 投稿时间：2023-04-27 修订日期：2023-05-29 |
| DOI：10.13400/j.cnki.cjmd.2025.02.005 |
| 中文关键词: 透明质酸 青蒿琥酯 纳米胶束 肿瘤细胞 |
| English Keywords:Hyaluronic acid Artesunate Nano-micelles Tumor cells |
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| 中文摘要: |
| 摘 要：目的 制备透明质酸/青蒿琥酯共聚物并对其抗结肠癌活性进行研究，为结肠癌治疗提供了新思路。方法 以透明质酸（HA）、青蒿琥酯（ART）为原料，通过酰胺化偶联反应制备糖-药物偶联物HA-ART，经超声制备纳米胶束，在对其形貌、临界胶束浓度等性能进行表征的基础上，进一步在分子和细胞水平对肿瘤细胞毒性进行评价。结果 糖-药物偶联物浓度在86 μg/mL时，形成粒径均一的纳米胶束，对肿瘤细胞有显著抑制作用。结论 HA-ART NPs呈现较好的pH依赖性，被肿瘤细胞广泛摄取，并表现出良好的抑制肿瘤细胞增殖的作用，与AT Ⅲ蛋白结合抑制NF-κB信号通路，具有开发成为新型抗肿瘤药物的潜力。 |
| English Summary: |
| Abstract: Objective To prepare hyaluronic acid/artesunate glycoconjugate and study its anti-colon cancer activity, providing a new method for the treatment of colon cancer. Methods Using hyaluronic acid (HA) and artesunate (ART) as raw materials, the carbohydrate-drug conjugate HA-ART was prepared by amidation coupling reaction. Nanomicelles were prepared by ultrasound. Based on the characterization of the morphology, critical micelle concentration performance, the cytotoxicity of tumor cells was evaluated at the molecular and cellular levels. Results When the concentration of carbohydrate-drug conjugation was 86 μg/mL, the nanomicelles with uniform particle size were formed, which showed significant inhibitory effect on tumor cells. Conclusion HA-ART NPs are significantly taken up by tumor cells in pH-dependent manner, and show good inhibitory effect on tumor cell proliferation. HA-ART NPs bind with AT-III protein to inhibit NF-κB signaling pathway, and exhibit the potential to be developed as novel antitumor drugs. |
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