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结构特征、硒化修饰及提高枇杷多糖抗肿瘤活性的研究。

Structure features, selenylation modification, and improved anti-tumor activity of a polysaccharide from Eriobotrya japonica.

机构信息

State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, Tianjin Key Laboratory of Molecular Drug Research, and Drug Discovery Center for Infectious Disease, Nankai University, Tianjin 300350, People's Republic of China.

College of Chemistry and Environmental Sciences, Laboratory of Xinjiang Native Medicinal and Edible Plant Resources Chemistry, Kashgar University, Kashgar 844000, People's Republic of China.

出版信息

Carbohydr Polym. 2021 Dec 1;273:118496. doi: 10.1016/j.carbpol.2021.118496. Epub 2021 Jul 29.

Abstract

A homogeneous polysaccharide, EJP90-1, was isolated from the leaves of E. japonica by hot water extraction in this study. EJP90-1 (7702 Da) was a heteropolysaccharide mainly consisting of →5)-linked-α-L-Araf-(1→, →4)-linked-β-D-Manp-(1→, →2,4)-linked-α-L-Rhap-(1→, →4)-linked-α-D-Xylp-(1→, →4)-linked-β-D-Galp-(1→, →2)-linked-β-D-Galp-(1→, →6)-linked-β-D-Glcp-(1→, α-D-Glcp-(4→, and t-linked-α-L-Araf. EJP90-1 was found to show moderate anti-tumor activity at the cellular level. In order to improve the anti-tumor activity and the potential applications of EJP90-1, a typical sodium selenite-nitric acid (NaSeO-HNO) modification on EJP90-1 was carried out. X-ray photoelectron spectroscopy (XPS) and energy dispersive spectrometer (EDS) analysis confirmed that Se was successfully introduced into the polymer chain of EJP90-1. The subsequent in vitro cytotoxicity evaluation showed the selenylation modification derivative (EJP90-1-Se) possessed significant antiproliferative activity against cancer cells (HepG2 and A549 cells) through inducing cell apoptosis. The anti-tumor activity of EJP90-1-Se was further confirmed by zebrafish models, which inhibited the proliferation and migration of HepG2 cells and the angiogenesis.

摘要

从该研究中可知,从甜叶悬钩子叶中用热水提取分离出一种均一的多糖,EJP90-1。EJP90-1(7702 Da)是一种杂多糖,主要由→5)-连接的-α-L-Araf-(1→、→4)-连接的-β-D-Manp-(1→、→2,4)-连接的-α-L-Rhap-(1→、→4)-连接的-α-D-Xylp-(1→、→4)-连接的-β-D-Galp-(1→、→2)-连接的-β-D-Galp-(1→、→6)-连接的-β-D-Glcp-(1→、α-D-Glcp-(4→和 t-连接的-α-L-Araf 组成。EJP90-1 在细胞水平上显示出中等的抗肿瘤活性。为了提高 EJP90-1 的抗肿瘤活性和潜在应用,对 EJP90-1 进行了典型的亚硒酸钠-硝酸(NaSeO-HNO)修饰。X 射线光电子能谱(XPS)和能量色散谱(EDS)分析证实,硒成功地引入了 EJP90-1 的聚合物链中。随后的体外细胞毒性评价表明,硒代修饰衍生物(EJP90-1-Se)通过诱导细胞凋亡,对癌细胞(HepG2 和 A549 细胞)具有显著的增殖抑制活性。EJP90-1-Se 的抗肿瘤活性进一步通过斑马鱼模型得到证实,该模型抑制了 HepG2 细胞的增殖和迁移以及血管生成。

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