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標題: Synthesis of dextran-(5-FU)-galactosamine conjugate through a tripeptide spacer group and its in vitro properties
作者: Guu, J.A.
Juang, T.M.
Hsiue, G.H.
Chiu, H.C.
關鍵字: dextran;polymeric prodrug;galactosamine;targeting;5-fluorouracil;enzymatically degradable bonds;co-polymers;lysosomal-enzymes;side-chains;n-(2-hydroxypropyl)methacrylamide;5-fluorouracil;recognition;copolymers;carriers;receptor
Project: Journal of the Chinese Institute of Chemical Engineers
期刊/報告no:: Journal of the Chinese Institute of Chemical Engineers, Volume 31, Issue 4, Page(s) 351-359.
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.
ISSN: 0368-1653
Appears in Collections:化學工程學系所

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