完整後設資料紀錄
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.author | Guu, JA | en_US |
dc.contributor.author | Juang, TM | en_US |
dc.contributor.author | Hsiue, GH | en_US |
dc.contributor.author | Chiu, HC | en_US |
dc.date.accessioned | 2014-12-08T15:45:05Z | - |
dc.date.available | 2014-12-08T15:45:05Z | - |
dc.date.issued | 2000-07-01 | en_US |
dc.identifier.issn | 0368-1653 | en_US |
dc.identifier.uri | http://hdl.handle.net/11536/30412 | - |
dc.description.abstract | In this study, conjugation of 5-fluorouracil (5-FU) and galactosamine with dextran via Glycyl-L-Leucyl-Glycine (Gly-Leu-Gly) tripeptidyl spacer was performed first by activation of dextran with p-nitrophenyl chloroformate, followed by aminolysis of Glycyl-L-Leucyl-Glycyl-5flurouracil (Gly-Leu-Gly-5-FU) and galactosamine with activated dextrans. Preparation of Gly-Leu-Gly-5-FU was carried out by sequential reactions of peptide synthesis in solution phases and coupling with 5-FU in the presence of diethylphosphoric cyanide. The release of 5-FU from the conjugates upon the exposure of polymeric prodrugs to papain implied that the attachment of 5-FU with the tripeptidyl spacer, Gly-Leu-Gly, was capable of being liberated by cathepsin B in lysosomes of targeted cells. The observation that the cytoxicity in vitro from the incubation of dextran-5-FU conjugate containing galactosamine residues with Hep-3B cells is higher than that in the void of galactosamine indicated the occurrence of specific binding of the targeting moieties with its receptors on cell membrane, leading to an enhanced cellular uptake of the conjugate via receptor-mediated endocytosis. | en_US |
dc.language.iso | en_US | en_US |
dc.subject | dextran | en_US |
dc.subject | polymeric prodrug | en_US |
dc.subject | galactosamine | en_US |
dc.subject | targeting | en_US |
dc.subject | 5-fluorouracil | en_US |
dc.title | Synthesis of dextran-(5-FU)-galactosamine conjugate through a tripeptide spacer group and its in vitro properties | en_US |
dc.type | Article | en_US |
dc.identifier.journal | JOURNAL OF THE CHINESE INSTITUTE OF CHEMICAL ENGINEERS | en_US |
dc.citation.volume | 31 | en_US |
dc.citation.issue | 4 | en_US |
dc.citation.spage | 351 | en_US |
dc.citation.epage | 359 | en_US |
dc.contributor.department | 應用化學系 | zh_TW |
dc.contributor.department | Department of Applied Chemistry | en_US |
dc.identifier.wosnumber | WOS:000089231400005 | - |
dc.citation.woscount | 0 | - |
顯示於類別: | 期刊論文 |