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Characterization, bioactivity and pharmacokinetic study of a novel carbohydrate-peptide polymer: glycol-split heparin-endostatin2 (GSHP-ES2)
Carbohydrate Polymers ( IF 11.2 ) Pub Date : 2018-11-22 , DOI: 10.1016/j.carbpol.2018.11.043
Feng Sun , Zhendong Wang , Zhifang Yang , Yan Li , Huifei Cui , Chunhui Liu , Dezong Gao , Fengshan Wang , Haining Tan

Endostatin (ES) has attracted considerable attention for the treatment of anti-angiogenesis-related disorders. An 11-amino-acid peptide (ES2, IVRRADRAAVP) from the amino terminal of ES is of interest because it is the main active fragment of ES. However, both ES and ES2 have a poor stability and a short half-life, and other disadvantages need to be further resolved. Thus, we conjugated ES2 to glycol-split heparin derivatives (GSHPs) to yield the polymer-peptide conjugate, GSHP-ES2. This study showed that GSHP-ES2 exhibited increased stability, a wider pH activity range, better inhibition of endothelial cell proliferation, migration and tube formation in vitro, better anti-angiogenic activity and a longer half-life in vivo compared with ES2. These results also indicate that GSHP-ES2 has good potential for the treatment of angiogenesis-related diseases, either alone or in combination with other chemicals.



中文翻译:

新型糖肽聚合物:乙二醇裂解的肝素-内皮抑素2(GSHP-ES2)的表征,生物活性和药代动力学研究

内皮抑素(ES)在抗血管生成相关疾病的治疗方面已引起广泛关注。来自ES氨基末端的11个氨基酸的肽段(ES2,IVRRADRAAVP)很受关注,因为它是ES的主要活性片段。但是,ES和ES2都具有较差的稳定性和较短的半衰期,还有其他缺点需要进一步解决。因此,我们将ES2与乙二醇拆分的肝素衍生物(GSHPs)共轭,以生成聚合物-肽共轭物GSHP-ES2。这项研究表明,GSHP-ES2在体外具有更高的稳定性,更宽的pH活性范围,更好的抑制内皮细胞增殖,迁移和管形成,更好的抗血管生成活性以及更长的体内半衰期与ES2相比。这些结果还表明,GSHP-ES2单独或与其他化学物质联合使用具有治疗血管新生相关疾病的良好潜力。

更新日期:2018-11-24
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