氨基葡萄糖修饰多柔比星靶向性研究
Targeted biodistribution of aminoglucose-modified doxorubicin
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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。
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关键词:
- 2-脱氧-氨基葡萄糖 /
- 多柔比星 /
- 修饰 /
- 靶向性
Abstract: In order to improve in vivotargeting 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.-
Keywords:
- 2-deoxy-aminoglucose /
- doxorubicin /
- modify /
- targeting
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