Enhanced anti-angiogenesis and anti-tumor activity of endostatin by chemical modification with polyethylene glycol and low molecular weight heparin

被引：11
作者：
Tan, Haining [1 ,2 ,3 ]
Yang, Shenglin [1 ]
Liu, Chunhui [1 ,2 ]
Cao, Jichao [1 ,2 ]
Mu, Guoying [4 ,5 ]
Wang, Fengshan [1 ,2 ]
机构：
[1] Shandong Univ, Sch Pharmaceut Sci, Inst Biochem & Biotechnol Drug, Jinan 250012, Peoples R China
[2] Shandong Univ, Natl Glycoengn Res Ctr, Jinan 250012, Peoples R China
[3] Shandong Univ, Sch Life Sci, Jinan 250012, Peoples R China
[4] Shandong Univ, Jinan Cent Hosp, Jinan 250012, Peoples R China
[5] Shandong Univ, Clin Med Coll, Jinan 250012, Peoples R China
来源：
BIOMEDICINE & PHARMACOTHERAPY | 2012年 / 66卷 / 08期
基金：
中国博士后科学基金; 中国国家自然科学基金;
关键词：
Anti-tumor activity; CAM assay; CNV assay; Modified endostatin; Sarcoma; 180; CHOROIDAL NEOVASCULARIZATION; SUPEROXIDE-DISMUTASE; TUMOR-GROWTH; INHIBITION; SUPPRESSION; THERAPY; CANCER;
D O I：
10.1016/j.biopha.2011.04.007
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
Endostatin (ES), a potent endogenous angiogenesis inhibitor found in 1997 by O'Reilly, can effectively inhibit angiogenesis, inhibit the growth and metastasis of tumors. ES can also decrease drug resistance in long term and repeated treatment when it is used in combination with other chemotherapeutic agents. But there are still lots of obstacles on its clinical application, such as the need of a high dose to maintain its efficacy short half-life, poor stability, expensive, and some other shortcomings just like other protein drugs. Chemical modification on ES by polyethylene glycol (PEG) and low molecular weight heparin (LMWH) were successfully carried out in order to obtain a better ES derivative. Several classic experimental models were employed to study the bioactivity of ES and modified ES, including chicken chorioallantoic membrane (CAM) assay, corneal neovascularization (CNV) assay and Sarcoma 180 tumor bearing mice assay. The results showed that PEG-ES and LMWH-ES had better anti-angiogenesis and anti-tumor activity than ES, which indicates that LMWH was also a good protein modifier. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：648 / 654
页数：7
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