氨基葡萄糖修饰多柔比星靶向性研究  

Targeted biodistribution of aminoglucose-modified doxorubicin

作　　者：李斯文[1] 田俊梅[1] 金靖[1] 杜长丽[1] 赵娟[1] 顾月清[1] 

机构地区：[1]中国药科大学生命科学与技术学院生物医学工程教研室,南京210009

出　　处：《中国药科大学学报》2012年第3期266-270,共5页Journal of China Pharmaceutical University

摘　　要：为了提高多柔比星(Dox)体内靶向性,降低毒副作用,将2-脱氧-氨基葡萄糖(AG)对多柔比星进行靶向配体修饰,形成一种全新抗肿瘤药物。对产物进行1H NMR、MS表征,运用近红外成像技术对产物靶向性进行研究,并通过MTT法比较产物与多柔比星对MCF-7细胞和U87MG细胞的药效作用。研究表明,与多柔比星相比,修饰过的产物靶向性和药效作用都有很大提高,具有很好的应用前景。In order to improve in vivo targeting of doxorubicin（Dox） and reduce its toxicity,the targeting ligand 2-deoxy-aminoglucose（AG） was used to modify doxorubicin to form a new anti-tumor drug.The products were charactered by 1H NMR and MS,and the targeting was investigated by near-infrared imaging.Compared with Dox,the product treating MCF-7 and U87MG cells showed higher antitumor activity in vitro by MTT assay.In conclusion,the modified products effectively enhanced the targeting and pharmacodynamics in contrast with Dox,and it would be a potential therapeutic drug for cancer.

关 键 词：2-脱氧-氨基葡萄糖 多柔比星 修饰 靶向性 

分 类 号：R914[医药卫生—药物化学]