Targeting the Delivery of Glycan-Based Paclitaxel Prodrugs to Cancer Cells via Glucose

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TMUIR > College of Biomedical Engineering > Graduate Institute of Biomedical Materials and Tissue Engineering > Periodical Article > Item 987654321/2460

Please use this identifier to cite or link to this item: http://libir.tmu.edu.tw/handle/987654321/2460

Title:	Targeting the Delivery of Glycan-Based Paclitaxel Prodrugs to Cancer Cells via Glucose
Authors:	劉得任 Yih-Shyan Lin;Rudeewan Tungpradit;Supachok Sinchaikul;Der-Zen Liu;Shui-Tein Chen
Contributors:	生醫材料暨工程研究所
Date:	2008
Issue Date:	2009-08-20 12:47:22 (UTC+8)
Abstract:	This report describes the synthesis of four novel paclitaxel based prodrugs with glycan conjugation (1-4). Glycans were conjugated using an ester or ether bond as the linker between 2'-paclitaxel and the 2'-glucose or glucuronic acid moiety. These prodrugs showed good water solubility and selective cytotoxicity against cancer cell lines, but showed reduced toxicity toward normal cell lines and cancer cell lines with low expression levels of GLUTs. The ester conjugated prodrug 1 showed the most cytotoxicity among the prodrugs examined and could be transported into cells via GLUTs. Fluorescent and confocal microscopy demonstrated that targeted cells exhibited morphological changes in tubulin and chromosomal alterations that were similar to those observed with paclitaxel treatment. Therefore, these glycan-based prodrugs may be good drug candidates for cancer therapy, and the glycan conjugation approach is an alternative method to enhance the targeted delivery of other drugs to cancer cells that overexpress GLUTs.
Relation:	J. Med. Chem.(2008):7428-7441.
Data Type:	article
Appears in Collections:	[Graduate Institute of Biomedical Materials and Tissue Engineering] Periodical Article

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