Six amphiphilic cholesterylated thiogalactosides la-f with high affinity for the asialoglycoprotein receptor have been synthesized by coupling 2,3,4,6-tetra -O-acetyl-l-thio-β-D-galactopyranose 8 with prepared choles...Six amphiphilic cholesterylated thiogalactosides la-f with high affinity for the asialoglycoprotein receptor have been synthesized by coupling 2,3,4,6-tetra -O-acetyl-l-thio-β-D-galactopyranose 8 with prepared cholesterol derivatives 7a-f, then by deacetylating. Preliminary results show liposomes containing those galactosides derivatives exhibited higher affinity and transfection activity in hepatoma cells HepG2 and SMMC-7721.展开更多
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 synthesize...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.展开更多
Prednisolone succinate-glucosamine（PSG） conjugate,a prodrug for prednisolone,was synthesized and confirmed by NMR and MS spectrum.The stabilities of the prodrug in PBS（pH 2.50,5.00,7.20,and 7.89） were studied.Cyto...Prednisolone succinate-glucosamine（PSG） conjugate,a prodrug for prednisolone,was synthesized and confirmed by NMR and MS spectrum.The stabilities of the prodrug in PBS（pH 2.50,5.00,7.20,and 7.89） were studied.Cytotoxicity and uptake assay of the prodrug were perfomed on HK-2 and MDCK cell lines.The results showed that compared with prednisolone,the PSG not only did not increase the cytotoxicity but also improved the uptake to 2.2 times of prednisolone by the cells.Thus,it indicated that glucosamine might be a potential carrier for kidney-targeting delivery of prednisolone.展开更多
基金This work was funded by the National High Technology Research and Development Program of China(863 program,No.2001AA218021).
文摘Six amphiphilic cholesterylated thiogalactosides la-f with high affinity for the asialoglycoprotein receptor have been synthesized by coupling 2,3,4,6-tetra -O-acetyl-l-thio-β-D-galactopyranose 8 with prepared cholesterol derivatives 7a-f, then by deacetylating. Preliminary results show liposomes containing those galactosides derivatives exhibited higher affinity and transfection activity in hepatoma cells HepG2 and SMMC-7721.
基金supported by the National Science & Technology Major Project of China(No2009ZX09310-002)
文摘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.
基金supported by the National Science & Technology Major Project of China(No.2009ZX09310- 002)
文摘Prednisolone succinate-glucosamine（PSG） conjugate,a prodrug for prednisolone,was synthesized and confirmed by NMR and MS spectrum.The stabilities of the prodrug in PBS（pH 2.50,5.00,7.20,and 7.89） were studied.Cytotoxicity and uptake assay of the prodrug were perfomed on HK-2 and MDCK cell lines.The results showed that compared with prednisolone,the PSG not only did not increase the cytotoxicity but also improved the uptake to 2.2 times of prednisolone by the cells.Thus,it indicated that glucosamine might be a potential carrier for kidney-targeting delivery of prednisolone.
