【作者】 谭海宁； 杨盛林； 刘纯慧； 曹吉超； 牟国营； 王凤山；

【Author】 Haining Tan 1,2, Shenglin Yang1, Chunhui Liu1,2, Jichao Cao1,2, Guoying Mu3, and Fengshan Wang1,2,* 1Institute of Biochemical and Biotechnological Drug, School of Pharmaceutical Science, Shandong University, Jinan; 2National Glycoengineering Research Center, Shandong University, Jinan; and 3Jinan Central Hospital and Clinical Medical College of Shandong University, Jinan,China

【机构】 山东大学药学院； 山东大学国家糖工程技术研究中心； Jinan Central Hospital and Clinical Medical College of Shandong University；

【摘要】 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 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 protein exhibit high heat stability, high percentage of retained activity and slight secondary structure alteration. This encouraged us to do the study on the anti-angiogenesis and anti-tumor activity of the modified products in vivo. Thus, chicken chorioallantoic membrane (CAM) assay, corneal neovascularization (CNV) assay and Sarcoma 180 tumor bearing mice assay were studied. And the results indicated that both PEG-ES and LMWH-ES had better anti-angiogenesis and anti-tumor activity than that of ES.更多还原

【Abstract】 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 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 protein exhibit high heat stability, high percentage of retained activity and slight secondary structure alteration. This encouraged us to do the study on the anti-angiogenesis and anti-tumor activity of the modified products in vivo. Thus, chicken chorioallantoic membrane (CAM) assay, corneal neovascularization (CNV) assay and Sarcoma 180 tumor bearing mice assay were studied. And the results indicated that both PEG-ES and LMWH-ES had better anti-angiogenesis and anti-tumor activity than that of ES.更多还原