标题：Characterization, bioactivity and pharmacokinetic study of a novel carbohydrate-peptide polymer: Glycol-split heparin-endostatin2 (GSHP-ES2)
作者：Sun, Feng; Wang, Zhendong; Yang, Zhifang; Li, Yan; Cui, Huifei; Liu, Chunhui; Gao, Dezong; Wang, Fengshan; Tan, Haining
作者机构：[Sun, Feng; Wang, Zhendong; Yang, Zhifang; Li, Yan; Tan, Haining] Shandong Univ, Natl Glycoengn Res Ctr, Jinan 250012, Shandong, Peoples R China.; [ 更多
通讯作者：Tan, Haining;Tan, HN
通讯作者地址：[Tan, HN]Shandong Univ, Natl Glycoengn Res Ctr, Jinan 250012, Shandong, Peoples R China.
关键词：Glycol-split heparin; ES2; Anti-angiogenesis; Zebra fish; Stability
摘要：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.