Polymer Research laboratory, Department of Chemistry, Motilal Nehru National Institute of Technology, Allahabad, 211004, India.
Polymer Research laboratory, Department of Chemistry, Motilal Nehru National Institute of Technology, Allahabad, 211004, India; Department of Chemical Engineering, Motilal Nehru National Institute of Technology, Allahabad, 211004, India.
Int J Biol Macromol. 2018 Apr 15;110:234-244. doi: 10.1016/j.ijbiomac.2017.11.002. Epub 2017 Nov 8.
In this study, we have synthesized chitin-glucan quercetin conjugate (ChGCQ) by an easy and facile free radical grafting reaction. The structure of ChGCQ was confirmed by proton nuclear magnetic resonance (H NMR) and Fourier transforms infrared spectroscopy (FT-IR). Curcumin was loaded into ChGCQ to study its anti-cancer efficiency. The biocompatibility of ChGCQ and curcumin loaded ChGCQ (Cu-ChGCQ) were analysed by different assays in Peripheral blood mononuclear cells (PBMCs) and cytotoxicity test was performed in a macrophage cancer cell line (J774). The result shows tremendous biocompatibility of ChGCQ and Cu-ChGCQ in peripheral blood mononuclear cells and excellent cytotoxity in macrophage cancer cell line (J774). Chitin-glucan complex (ChGC), ChGCQ and Cu-ChGCQ showed 51%, 66% and 74% of DPPH radical-scavenging activity at 1mg/ml respectively, which are much higher than that of ChGC and in ABTS* assay 58%, 71% and 83% show radical-scavenging activity at 1mg/ml. Antioxidant assay of Cu-ChGCQ conjugate expressed much higher antioxidant activity than ChGCQ and ChGC. In vitro drug release study of Cu-ChGCQ conjuagate showed faster drug release in acidic medium in comparison to PBS of physiological pH and anticancer activity in vitro assay showed more anticancer activity of Cu-ChGCQ in comparison to ChGCQ conjugate.
在这项研究中，我们通过简单易行的自由基接枝反应合成了壳聚糖-葡聚糖槲皮素缀合物（ChGCQ）。ChGCQ 的结构通过质子核磁共振（1H NMR）和傅里叶变换红外光谱（FT-IR）得到证实。姜黄素被载入 ChGCQ 以研究其抗癌效率。ChGCQ 和负载姜黄素的 ChGCQ（Cu-ChGCQ）的生物相容性通过外周血单个核细胞（PBMCs）中的不同测定进行分析，并在巨噬细胞癌细胞系（J774）中进行细胞毒性试验。结果表明，ChGCQ 和 Cu-ChGCQ 在外周血单个核细胞中具有极好的生物相容性，在巨噬细胞癌细胞系（J774）中具有优异的细胞毒性。壳聚糖-葡聚糖复合物（ChGC）、ChGCQ 和 Cu-ChGCQ 在 1mg/ml 时分别表现出 51%、66%和 74%的 DPPH 自由基清除活性，均明显高于 ChGC，在 ABTS*测定中，在 1mg/ml 时分别表现出 58%、71%和 83%的自由基清除活性。Cu-ChGCQ 缀合物的抗氧化测定表明，其抗氧化活性明显高于 ChGCQ 和 ChGC。体外药物释放研究表明，与生理 pH 的 PBS 相比，Cu-ChGCQ 缀合物在酸性介质中具有更快的药物释放，体外抗癌活性研究表明，与 ChGCQ 缀合物相比，Cu-ChGCQ 具有更强的抗癌活性。
