基于鼠李糖半乳糖醛酸 I 的新型两亲性纳米细胞,用于向肝癌细胞靶向输送姜黄素

IF 2.7 3区 化学 Q2 POLYMER SCIENCE Journal of Applied Polymer Science Pub Date : 2024-09-16 DOI:10.1002/app.56264
Yuejiao Wu, Jian Yang, Ke Shen, Liyan Liu, Jing Cao, Zhaomei Wang
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引用次数: 0

摘要

姜黄素(Cur)是一种具有生物活性的营养保健品,在生物、营养和医疗方面具有巨大的应用潜力。然而,这些应用受到各种因素的限制,如摄入量不足、水溶性低以及对正常细胞的毒性相对较高。为了解决这些障碍,我们合成了一种新型的 Cur 改性鼠李糖半乳糖醛酸(RG-C)纳米胶束载体,通过过表达的表面半乳糖苷-3 受体对 RG-I 的特异性识别,将 Cur 靶向递送至肝癌 HepG2 细胞。傅立叶变换红外光谱、紫外-可见光谱和 1H NMR 分析证实了 RG 与 Cur 之间的共轭作用,负载 Cur 的 RG-CC 在水溶液中通过自组装形成,药物负载效率为 12.2%。通过扫描电子显微镜观察,RG-CC 胶束呈椭圆形或立方体,大小在 100 至 200 纳米之间。RG-CC 的咖 啡释放量与 pH 值有关,在 pH 值为 5.0 时,咖啡释放量为 50%,而在 pH 值为 7.4 时,咖啡释放量为 5%。与正常胚胎肾脏 293T 细胞相比,RG-CC 对 HepG2 细胞具有更强的抗增殖活性。激光共聚焦显微镜和流式细胞术分析表明,与游离 Cur 相比,RG-CC 在 HepG2 细胞中的抗增殖效果和吸收率都明显更高。RG-CC 是一种很有前景的抗癌候选化合物,值得进一步进行临床前和临床研究。
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Novel amphiphilic rhamnogalacturonnan I-based nanomicelles for targeted delivery of curcumin to hepatocellular carcinoma cells

Curcumin (Cur) is a bioactive nutraceutical with great potential in biological, nutritional, and medical applications. However, these applications are limited by various factors such as insufficient ingestion, low aqueous solubility, and relatively high toxicity to normal cells. To tackle these obstacles, we synthesized a novel Cur-modified-rhamnogalacturonan (RG-C) nano-micelle carrier to target-deliver Cur to hepatocellular carcinoma HepG2 cells via specific recognition of RG-I by the overexpressed surface galactin-3 receptor. Fourier transfer infrared, UV–vis, and 1H NMR analyses confirmed the conjugation between RG and Cur RG-C loaded with Cur (RG-CC) was formed via self-assembly in an aqueous solution with a drug loading efficiency of 12.2%. RG-CC micelle was ellipsoidal or cubic with a size ranging between 100 and 200 nm by scanning electron microscopy observation. Cur release from RG-CC exhibited a controlled and pH-dependent manner with 50% at pH 5.0 in contrast to 5% at pH 7.4 after 24 h exposure. RG-CC possessed more potent anti-proliferative activity against HepG2 cells than normal embryonic kidney 293T cells. Compared to free Cur, both the anti-proliferative effect and uptake of RG-CC were significantly higher in HepG2 cells as revealed from laser confocal microscopy and flow cytometry analyses. RG-CC was a promising anticancer candidate and deserves further preclinical and clinical investigations.

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来源期刊
Journal of Applied Polymer Science
Journal of Applied Polymer Science 化学-高分子科学
CiteScore
5.70
自引率
10.00%
发文量
1280
审稿时长
2.7 months
期刊介绍: The Journal of Applied Polymer Science is the largest peer-reviewed publication in polymers, #3 by total citations, and features results with real-world impact on membranes, polysaccharides, and much more.
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Editorial Board, Aims & Scope, Table of Contents Editorial Board, Aims & Scope, Table of Contents Editorial Board, Aims & Scope, Table of Contents Editorial Board, Aims & Scope, Table of Contents Synthesis of reaction promoters for epoxy polymerization: Enhancing storage stability and mechanical properties of one-pot epoxy systems
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