首页> 中文会议>2009年中国药学大会暨第九届中国药师周 >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

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

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 tomaintain 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.

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