Synthesis and in vivo distribution of 2-deoxy-2-aminodiglucose-prednisolone conjugate(DPC)  

作　　者：Yan Lin Xun Sun Tao Gong Zhi Rong Zhang 

机构地区：[1]Key Laboratory of Drug Targeting of Ministry of Education,West China School of Pharmacy,Sichuan University,Chengdu 610041,China

出　　处：《Chinese Chemical Letters》2012年第5期557-560,共4页中国化学快报（英文版）

基　　金：supported by the National Science & Technology Major Project of China(No2009ZX09310-002)

摘　　要：In order to develop a novel kidney-targeted drug delivery system,a small molecular carrier（2-deoxy-2-aminodiglucose） was synthesized,and then the 2-deoxy-2-aminodiglucose-prednisolone conjugate（DPC） was synthesized to verify the kidney targeting capability of the carrier.Both 2-deoxy-2-aminodiglucose and DPC were confirmed by NMR and MS spectrum.The tissue distribution studies showed that DPC presented an excellent kidney targeting property in vivo,compared with prednisolone group, 4.9-fold of drug concentration in kidney was observed in the DPC group.Thus,it indicated that 2-deoxy-2-aminodiglucose could be a potential carrier for kidney-targeted drug delivery.In order to develop a novel kidney-targeted drug delivery system,a small molecular carrier（2-deoxy-2-aminodiglucose） was synthesized,and then the 2-deoxy-2-aminodiglucose-prednisolone conjugate（DPC） was synthesized to verify the kidney targeting capability of the carrier.Both 2-deoxy-2-aminodiglucose and DPC were confirmed by NMR and MS spectrum.The tissue distribution studies showed that DPC presented an excellent kidney targeting property in vivo,compared with prednisolone group, 4.9-fold of drug concentration in kidney was observed in the DPC group.Thus,it indicated that 2-deoxy-2-aminodiglucose could be a potential carrier for kidney-targeted drug delivery.

关 键 词：SYNTHESIS 2-Deoxy-2-aminodiglucose PREDNISOLONE Tissue distribution 

分 类 号：TQ467.8[化学工程—制药化工] S562.01[农业科学—作物学]