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基于葡聚糖醛和 BSA 的酚类化合物缀合物的制备、表征及其在治疗中的抗癌功效评价。

Phenolic compounds based conjugates from dextran aldehyde and BSA: Preparation, characterization and evaluation of their anti-cancer efficacy for therapeutic applications.

机构信息

Department of Chemistry, Motilal Nehru National Institute of Technology Allahabad, Allahabad, 211004, India, India.

Department of Biotechnology, Motilal Nehru National Institute of Technology Allahabad, Allahabad, 211004, India.

出版信息

Int J Biol Macromol. 2018 Apr 15;110:425-436. doi: 10.1016/j.ijbiomac.2017.11.049. Epub 2017 Nov 10.

Abstract

Here, we have synthesized phenolic compounds (pc) based on conjugates from dextran aldehyde (dex-ald) and bovine serum albumin (BSA) and screening their potential activity as therapeutic agents in cancer disease. The synthesized conjugates were analyzed by UV-vis, FT-IR, XRD and SEM analysis. UV-vis spectra of conjugates showed the shifting of spectral peak at UV to visible region revealed the enhanced conjugation due to formation of linkage. The XRD peaks of conjugates found broader and indicating the amorphous phase of conjugating materials in compared to free components. The SEM images showed that the conjugated materials having numerous pores on its surface, which proved its porous nature. The amount of phenolic compounds conjugated with (dex-ald-pc) and (BSA-pc) were found to be 65.4 and 73.91mg/g of conjugates, respectively. Cells viability was significantly decreased approximately 80-85% at concentration of 100μg conjugates whereas the free polymers or phenolics did not affect the viability of cancer cells. Generation of high quantity of reactive oxygen species (ROS) in cells treated with conjugate materials, which may caused cell apoptosis in cancer cell line. The results clearly showed that conjugation of phenolic compounds were an effective method to improve the functional properties for therapeutic applications.

摘要

在这里,我们合成了基于葡聚糖醛(dex-ald)和牛血清白蛋白(BSA)缀合物的酚类化合物(pc),并筛选了它们作为癌症治疗药物的潜在活性。通过 UV-vis、FT-IR、XRD 和 SEM 分析对合成的缀合物进行了分析。缀合物的 UV-vis 光谱显示,UV 光谱峰向可见区域的移动表明由于形成键合,共轭增强。与游离组分相比,缀合物的 XRD 峰发现更宽,表明结合材料的非晶相。SEM 图像显示,接合物表面有许多孔,证明其具有多孔性。与(dex-ald-pc)和(BSA-pc)缀合的酚类化合物的量分别为 65.4 和 73.91mg/g 缀合物。在 100μg 缀合物浓度下,细胞活力显著降低约 80-85%,而游离聚合物或酚类化合物对癌细胞活力没有影响。在用缀合材料处理的细胞中产生了大量的活性氧物种(ROS),这可能导致癌细胞系中的细胞凋亡。结果清楚地表明,酚类化合物的缀合是提高治疗应用功能特性的有效方法。

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