PDF(Pubmed)
Abstract：
UNASSIGNED: Vitamin E, which is also known as tocopherol, is a compound with a polyphenol structure. Its esterified derivative, Vitamin E succinate (VES), exhibits unique anticancer and healthcare functions as well as immunomodulatory effects. Natural polysaccharides are proved to be a promising material for nano-drug delivery systems, which show excellent biodegradability and biocompatibility. In this study, we employed a novel bletilla striata polysaccharide-vitamin E succinate polymer (BSP-VES) micelles to enhance the tumor targeting and anti-colon cancer effect of andrographolide (AG).
UNASSIGNED: BSP-VES polymer was synthesized through esterification and its structure was confirmed using 1H NMR. AG@BSP-VES was prepared via the dialysis method and the drug loading, entrapment efficiency, stability, and safety were assessed. Furthermore, the tumor targeting ability of AG@BSP-VES was evaluated through targeted cell uptake and in vivo imaging. The antitumor activity of AG@BSP-VES was measured in vitro using MTT assay, Live&Dead cell staining, and cell scratch test.
UNASSIGNED: In this study, we successfully loaded AG into BSP-VES micelles (AG@BSP-VES), which exhibited good stability, biosafety and sustained release effect. In addition, AG@BSP-VES also showed excellent internalization capability into CT26 cells compared with NCM460 cells in vitro. Meanwhile, the specific delivery of AG@BSP-VES micelles into subcutaneous and in-situ colon tumors was observed compared with normal colon tissues in vivo during the whole experiment process (1-24 h). What\'s more, AG@BSP-VES micelles exhibited significant antitumor activities than BSP-VES micelles and free AG.
UNASSIGNED: The study provides a meaningful new idea and method for application in drug delivery system and targeted treatment of colon cancer based on natural polysaccharides.
UNASSIGNED: BSP-VES polymer was synthesized through esterification and its structure was confirmed using 1H NMR. AG@BSP-VES was prepared via the dialysis method and the drug loading, entrapment efficiency, stability, and safety were assessed. Furthermore, the tumor targeting ability of AG@BSP-VES was evaluated through targeted cell uptake and in vivo imaging. The antitumor activity of AG@BSP-VES was measured in vitro using MTT assay, Live&Dead cell staining, and cell scratch test.
UNASSIGNED: In this study, we successfully loaded AG into BSP-VES micelles (AG@BSP-VES), which exhibited good stability, biosafety and sustained release effect. In addition, AG@BSP-VES also showed excellent internalization capability into CT26 cells compared with NCM460 cells in vitro. Meanwhile, the specific delivery of AG@BSP-VES micelles into subcutaneous and in-situ colon tumors was observed compared with normal colon tissues in vivo during the whole experiment process (1-24 h). What\'s more, AG@BSP-VES micelles exhibited significant antitumor activities than BSP-VES micelles and free AG.
UNASSIGNED: The study provides a meaningful new idea and method for application in drug delivery system and targeted treatment of colon cancer based on natural polysaccharides.
摘要：
■维生素E，也被称为生育酚，是具有多酚结构的化合物。其酯化衍生物，维生素E琥珀酸酯（VES），具有独特的抗癌和保健功能以及免疫调节作用。天然多糖被证明是一种有前途的纳米药物传递系统的材料，表现出优异的生物降解性和生物相容性。在这项研究中,我们采用了一种新型白杨多糖-维生素E琥珀酸酯聚合物（BSP-VES）胶束来增强穿心莲内酯（AG）的肿瘤靶向和抗结肠癌作用。
■BSP-VES聚合物通过酯化合成,并且其结构使用1HNMR确认。通过透析法和载药法制备AG@BSP-VES，截留效率，稳定性,和安全性进行了评估。此外，通过靶向细胞摄取和体内成像评估AG@BSP-VES的肿瘤靶向能力。用MTT法测定AG@BSP-VES的体外抗肿瘤活性,活细胞和死细胞染色，和细胞划痕测试。
■在这项研究中，我们成功地将AG加载到BSP-VES胶束（AG@BSP-VES）中，表现出良好的稳定性，生物安全性和缓释效果。此外,与体外NCM460细胞相比,AG@BSP-VES还显示出优异的内化能力进入CT26细胞。同时,在整个实验过程中（1-24h），与体内正常结肠组织相比，观察到AG@BSP-VES胶束向皮下和原位结肠肿瘤的特异性递送。更重要的是，AG@BSP-VES胶束比BSP-VES胶束和游离AG具有显著的抗肿瘤活性。
■该研究为基于天然多糖的药物传递系统和结肠癌的靶向治疗提供了有意义的新思路和方法。
■BSP-VES聚合物通过酯化合成,并且其结构使用1HNMR确认。通过透析法和载药法制备AG@BSP-VES，截留效率，稳定性,和安全性进行了评估。此外，通过靶向细胞摄取和体内成像评估AG@BSP-VES的肿瘤靶向能力。用MTT法测定AG@BSP-VES的体外抗肿瘤活性,活细胞和死细胞染色，和细胞划痕测试。
■在这项研究中，我们成功地将AG加载到BSP-VES胶束（AG@BSP-VES）中，表现出良好的稳定性，生物安全性和缓释效果。此外,与体外NCM460细胞相比,AG@BSP-VES还显示出优异的内化能力进入CT26细胞。同时,在整个实验过程中（1-24h），与体内正常结肠组织相比，观察到AG@BSP-VES胶束向皮下和原位结肠肿瘤的特异性递送。更重要的是，AG@BSP-VES胶束比BSP-VES胶束和游离AG具有显著的抗肿瘤活性。
■该研究为基于天然多糖的药物传递系统和结肠癌的靶向治疗提供了有意义的新思路和方法。
