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浒苔中一种硫酸化的葡糖醛酸木糖鼠李半乳聚糖的结构特征及其抗肺癌活性。

Structural characterization and anti-lung cancer activity of a sulfated glucurono-xylo-rhamnan from Enteromorpha prolifera.

机构信息

College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou, 310014, China; Department of Chemical and Biological Engineering, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, NY, 12180, USA.

College of Biotechnology and Bioengineering, Zhejiang University of Technology, Hangzhou, 310014, China.

出版信息

Carbohydr Polym. 2020 Jun 1;237:116143. doi: 10.1016/j.carbpol.2020.116143. Epub 2020 Mar 9.

DOI:10.1016/j.carbpol.2020.116143
PMID:32241440
Abstract

A sulfated glucurono-xylo-rhamnan (EP-3-H) was purified from a green alga, Enteromorpha prolifera. EP-3-H and its oligomers were characterized by high performance liquid chromatography, mass spectrometry and one and two-dimensional nuclear magnetic resource spectroscopy. The structural analysis showed EP-3-H has a backbone of glucurono-xylo-rhamnan, branches with glucuronic acid and sulfated at C3 of rhamnose and/or C2 of xylose. The inhibition of EP-3-H on human lung cancer A549 cell proliferation in vitro and its therapeutic effects in BALB/c-nu mice in vivo were determined to evaluate the anti-lung cancer activity of EP-3-H. The tumor inhibition level was 59 %, suggesting that EP-3-H might be a good candidate for the treatment of lung cancer. Surface plasmon resonance (SPR) studies revealed the IC on the binding of fibroblast growth factors, (FGF1 and FGF2), to heparin were 0.85 and 1.47 mg/mL, respectively. These results suggest that EP-3-H inhibits cancer proliferation by interacting with these growth factors.

摘要

一种硫酸化的葡醛酸-木糖-鼠李半乳聚糖(EP-3-H)从绿藻浒苔中分离得到。通过高效液相色谱、质谱和一维、二维核磁共振波谱对 EP-3-H 及其低聚物进行了表征。结构分析表明,EP-3-H 具有葡醛酸-木糖-鼠李半乳聚糖的骨架,分支为葡萄糖醛酸,在鼠李糖的 C3 和/或木糖的 C2 位硫酸化。体外测定 EP-3-H 对人肺癌 A549 细胞增殖的抑制作用及其在 BALB/c-nu 小鼠体内的治疗效果,以评估 EP-3-H 的抗肺癌活性。肿瘤抑制水平为 59%,表明 EP-3-H 可能是治疗肺癌的良好候选药物。表面等离子体共振(SPR)研究表明,EP-3-H 与肝素结合的纤维母细胞生长因子(FGF1 和 FGF2)的 IC 分别为 0.85 和 1.47mg/mL。这些结果表明,EP-3-H 通过与这些生长因子相互作用抑制肿瘤增殖。

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