School of Food Science and Engineering, South China University of Technology, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, Guangzhou 510640, China.
School of Food Science and Engineering, South China University of Technology, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, Guangzhou 510640, China; Sericultural & Agri-Food Research Institute, Guangdong Academy of Agricultural Sciences, Key Laboratory of Functional Foods, Ministry of Agriculture, Guangdong Key Laboratory of Agricultural Products Processing, Guangzhou 510610, China.
Int J Biol Macromol. 2020 Apr 15;149:672-681. doi: 10.1016/j.ijbiomac.2020.01.189. Epub 2020 Jan 22.
To preserve bioactivity and achieve colon targeted release of phycocyanin (PC), the polysaccharides-based electrospun fiber mat (EFM) containing PC and prebiotics was prepared and characterized. In vitro release tests confirmed the colon targeting behavior of PC, in particular, faster release of PC was achieved due to the addition of prebiotics. Ritger-Peppas model confirmed that the release of PC in simulated colon fluids follows a mechanism of anomalous transport (non-Fickian). CCK-8 results showed that the combination of PC and prebiotics exerted a significant anti-proliferative effect on HCT116 cells with an IC50 values of 22.31, 17.12 and 11.63 mg/mL after 24, 48, and 72 h, respectively. Furthermore, the cell cycle and apoptosis analysis revealed that the inhibition activity on HCT116 cells was caused by arresting cell cycle at G0/G1 phase that is relevant to the inhibition of cyclin D1 and CDK4 and the up-regulation of p21 expression, and inducing cell apoptosis by mediating the mitochondrial pathway as well, in which the decrease of Bcl-2/Bax, activation of caspase 3 and release of cytochrome c were included. This study suggests that the PC-loaded EFM with GOS holds a great potential as an effective formulation for colon cancer prevention.
为了保持藻蓝蛋白 (PC) 的生物活性并实现结肠靶向释放，制备并表征了含有 PC 和益生元的基于多糖的静电纺纤维垫 (EFM)。体外释放试验证实了 PC 的结肠靶向行为，特别是由于添加了益生元，实现了 PC 的更快释放。Ritger-Peppas 模型证实，PC 在模拟结肠液中的释放遵循异常传递机制（非菲克定律）。CCK-8 结果表明，PC 与益生元的组合对 HCT116 细胞表现出显著的抗增殖作用，在 24、48 和 72 h 时，IC50 值分别为 22.31、17.12 和 11.63 mg/mL。此外，细胞周期和凋亡分析表明，对 HCT116 细胞的抑制活性是通过将细胞周期阻滞在 G0/G1 期引起的，这与细胞周期蛋白 D1 和 CDK4 的抑制以及 p21 表达的上调有关，并通过介导线粒体途径诱导细胞凋亡，其中包括 Bcl-2/Bax 的减少、caspase 3 的激活和细胞色素 c 的释放。本研究表明，载有 GOS 的 PC 负载 EFM 作为结肠癌预防的有效制剂具有很大的潜力。
