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新型海藻糖糖醛酸钒配合物的合成、表征及生物学活性

Novel vanadyl complexes of alginate saccharides: synthesis, characterization, and biological activities.

机构信息

Yantai Institute of Coastal Zone Research Chinese Academy of Sciences, Yantai 264003, China; University of Chinese Academy of Sciences, Beijing 100049, China.

Yantai Institute of Coastal Zone Research Chinese Academy of Sciences, Yantai 264003, China.

出版信息

Carbohydr Polym. 2015 May 5;121:86-91. doi: 10.1016/j.carbpol.2014.11.069. Epub 2014 Dec 31.

DOI:10.1016/j.carbpol.2014.11.069
PMID:25659675
Abstract

Vanadium compounds present many physiological functions. However, vanadium(IV) and (V) salts are difficult for gastrointestinal absorption and have strong side effects. Therefore organic oxovanadium compounds gain more attention. Vanadyl alginate polysaccharides (VAPS) and vanadyl alginate oligosaccharides (VAOS) were obtained from aqueous solutions of VOSO4 at pH 12. They were characterized by infrared spectroscopy, UV-vis spectroscopy and inductively coupled plasma-mass spectrometry (ICP-MS). The antioxidant activity of oxovanadium(IV) complexes was investigated in hydroxyl and DPPH radical scavenging systems in vitro. The results reveal that activities of VAPS and VAOS in the two systems were stronger than those of alginate polysaccharides (APS) and alginate oligosaccharides (AOS), respectively. In addition, VAPS and VAOS promoted significantly the antiproliferation of ligands of human hepatoma cell line BEL-7402. Oxovanadium(IV) complexes were potent inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the range of 6.4-18.7μg/mL, indicated in biochemical assays. In addition, Vanadyl-alginate had no significant side effects on proliferation and viability of HL-7702 hepatic cells. In the future, they can be added to medicines and ease the growing threat that cancer and diabetes mellitus cause to human health.

摘要

钒化合物具有许多生理功能。然而,四价和五价钒盐难以被胃肠道吸收,且具有较强的副作用。因此,有机氧钒化合物受到了更多的关注。从 VOSO4 在 pH 12 的水溶液中可以得到藻酸钠多糖(VAPS)和藻酸钠低聚糖(VAOS)。通过红外光谱、紫外可见光谱和电感耦合等离子体质谱(ICP-MS)对它们进行了表征。在体外羟基和 DPPH 自由基清除体系中研究了氧钒(IV)配合物的抗氧化活性。结果表明,VAPS 和 VAOS 在这两个体系中的活性均强于藻酸钠多糖(APS)和藻酸钠低聚糖(AOS)。此外,VAPS 和 VAOS 显著促进了人肝癌细胞系 BEL-7402 配体的增殖。氧钒(IV)配合物对蛋白酪氨酸磷酸酶 1B(PTP1B)具有抑制作用,在生化测定中,IC50 值在 6.4-18.7μg/mL 范围内。此外,藻酸钠-钒对 HL-7702 肝细胞的增殖和活力没有显著的副作用。在未来,它们可以被添加到药物中,缓解癌症和糖尿病对人类健康造成的日益严重的威胁。

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