聚乙二醇及低分子肝素修饰内皮抑素的抗新生血管生成和抗肿瘤活性研究.pdfVIP

Anti-Angiogenesis and Anti-Tumor Activity of Endostatin Covalently Modified by Polyethylene Glycol and Low Molecular Weight Heparin 1,2 1 1,2 1,2 3 Haining Tan , Shenglin Yang , Chunhui Liu , Jichao Cao , Guoying Mu , and Fengshan Wang1,2,* 1 Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Science, Shandong 2 University, Jinan; National Glycoengineering Research Center, Shandong University, Jinan; and 3 Jinan Central Hospital and Clinical Medical College of Shandong University, Jinan,China Running title: Activity study on endostatin modification by PEG and LMWH 聚乙二醇及低分子肝素修饰内皮抑素的抗新生血管生成和抗肿瘤活性研究 谭海宁，杨盛林，刘纯慧，曹吉超，牟国营，王凤山 山东大学药学院 山东大学国家糖工程技术研究中心 Endostatin (ES), a potent endogenous angiogenesis inhibitor found in 1997 by O’Reilly, has been approved by the State Food and Drug Administration (SFDA) in China for the treatment of * To whom correspondence should be addressed. Tel: 86-531 Fax: 86-531 E-mail: fswang@sdu.edu.cn Abbreviations: ES, endostatin; PEG, polyethylene glycol; LMWH, low molecular weight heparin; CAM, chicken chorioallantoic membrane; CNV, corneal neovascularization; VEGF, vascular endothelial cell growth factor. 1 patients with non-small-cell lung cancer. But some obstacles such as need of high dose to maintain its efficacy, expensive, and poor stability inhibit its clinical use. In our previous study, 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. And the modified