Camptothecin delivery into hepatoma cell line by galactose-appended fluorescent drug delivery system

Sun Dongbang; Hyun Mi Jeon; Min Hee Lee; Weon Sup Shin; Joon Kook Kwon; Chulhun Kang; Jong Seung Kim

doi:10.1039/c4ra02588a

Camptothecin delivery into hepatoma cell line by galactose-appended fluorescent drug delivery system

Sun Dongbang, Hyun Mi Jeon, Min Hee Lee, Weon Sup Shin, Joon Kook Kwon, Chulhun Kang, Jong Seung Kim

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

Abstract

A galactose-appended camptothecin prodrug was newly synthesized. The prodrug preferentially entered a hepatoma cell line due to the galactose unit and the drug release triggered by disulfide-bond cleavage via reaction with glutathione was visualized on the basis of fluorescence changes of the naphthalimide moiety. The prodrug entered the cells via receptor-mediated endocytosis and released drug molecules into lysosomes, however, the released drug molecules failed to show significant anticancer activity, probably due to lysosomal hydrolysis of their lactone ring converting them to an inactive carboxylate form.

Original language	English
Pages (from-to)	18744-18748
Number of pages	5
Journal	RSC Advances
Volume	4
Issue number	36
DOIs	https://doi.org/10.1039/c4ra02588a
Publication status	Published - 2014

ASJC Scopus subject areas

Chemistry(all)
Chemical Engineering(all)

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abstract = "A galactose-appended camptothecin prodrug was newly synthesized. The prodrug preferentially entered a hepatoma cell line due to the galactose unit and the drug release triggered by disulfide-bond cleavage via reaction with glutathione was visualized on the basis of fluorescence changes of the naphthalimide moiety. The prodrug entered the cells via receptor-mediated endocytosis and released drug molecules into lysosomes, however, the released drug molecules failed to show significant anticancer activity, probably due to lysosomal hydrolysis of their lactone ring converting them to an inactive carboxylate form.",

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AU - Dongbang, Sun

AU - Jeon, Hyun Mi

AU - Lee, Min Hee

AU - Shin, Weon Sup

AU - Kwon, Joon Kook

AU - Kang, Chulhun

AU - Kim, Jong Seung

PY - 2014

Y1 - 2014

N2 - A galactose-appended camptothecin prodrug was newly synthesized. The prodrug preferentially entered a hepatoma cell line due to the galactose unit and the drug release triggered by disulfide-bond cleavage via reaction with glutathione was visualized on the basis of fluorescence changes of the naphthalimide moiety. The prodrug entered the cells via receptor-mediated endocytosis and released drug molecules into lysosomes, however, the released drug molecules failed to show significant anticancer activity, probably due to lysosomal hydrolysis of their lactone ring converting them to an inactive carboxylate form.

AB - A galactose-appended camptothecin prodrug was newly synthesized. The prodrug preferentially entered a hepatoma cell line due to the galactose unit and the drug release triggered by disulfide-bond cleavage via reaction with glutathione was visualized on the basis of fluorescence changes of the naphthalimide moiety. The prodrug entered the cells via receptor-mediated endocytosis and released drug molecules into lysosomes, however, the released drug molecules failed to show significant anticancer activity, probably due to lysosomal hydrolysis of their lactone ring converting them to an inactive carboxylate form.

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DO - 10.1039/c4ra02588a

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JO - RSC Advances

JF - RSC Advances

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ER -

Camptothecin delivery into hepatoma cell line by galactose-appended fluorescent drug delivery system

Abstract

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