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壳聚糖-葡聚糖-醛-槲皮素缀合物的合成及抗肿瘤和抗氧化活性评价。

Synthesis of chitin-glucan-aldehyde-quercetin conjugate and evaluation of anticancer and antioxidant activities.

机构信息

Polymer Research Laboratory, Department of Chemistry, India.

Polymer Research Laboratory, Department of Chemistry, India.

出版信息

Carbohydr Polym. 2018 Aug 1;193:99-107. doi: 10.1016/j.carbpol.2018.03.092. Epub 2018 Mar 27.

Abstract

In the present study, we have synthesized chitin-glucan-aldehyde-quercetin (chi-glu-ald-que) conjugate via condensation reaction. Synthesis of chitin-glucan-aldehyde (chi-glu-ald) complex was facilitated by the oxidation of chitin-glucan (chi-glu) complex. Formation of conjugate was confirmed by Proton nuclear magnetic resonance spectroscopy (H NMR) and Fourier-transform infrared spectroscopy (FT-IR). Morphological studies showed that after grafting of quercetin, several changes on surface were depicted and a more crystalline nature was observed. The chi-glu-ald-que conjugate displayed strong antioxidant activity. It showed 69% of 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical, DPPH* scavenging activity at 1 mg/mL and 72% of 2, 2-azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical cation, ABTS* scavenging activity at 1 mg/mL concentration, which are much higher than that of chi-glu complex. The anticancer activity of chi-glu-ald-que conjugate was performed in Macrophage cancer cell lines (J774) and biocompatibility was performed in Peripheral blood mononuclear cells (PBMCs). The chi-glu-ald-que conjugate showed excellent cytotoxicity against J774 cell lines but no cytotoxicity towards PBMCs.

摘要

在本研究中,我们通过缩合反应合成了几丁质-葡聚糖-醛-槲皮素(chi-glu-ald-que)缀合物。几丁质-葡聚糖(chi-glu)复合物的氧化促进了几丁质-葡聚糖-醛(chi-glu-ald)复合物的合成。质子核磁共振波谱(H NMR)和傅里叶变换红外光谱(FT-IR)证实了缀合物的形成。形态学研究表明,接枝槲皮素后,表面发生了一些变化,观察到更具结晶性。chi-glu-ald-que 缀合物表现出很强的抗氧化活性。在 1mg/mL 浓度下,它对 1,1-二苯基-2-苦基肼(DPPH)自由基的清除率达到 69%,对 2,2-偶氮双-(3-乙基苯并噻唑啉-6-磺酸)(ABTS)自由基阳离子的清除率达到 72%,均高于 chi-glu 复合物。chi-glu-ald-que 缀合物的抗癌活性在巨噬细胞癌细胞系(J774)中进行了评估,生物相容性在外周血单核细胞(PBMCs)中进行了评估。chi-glu-ald-que 缀合物对 J774 细胞系表现出优异的细胞毒性,但对 PBMCs 无细胞毒性。

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