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ChemComm
Page 4 of 5
DOI: 10.1039/C7CC04932C
COMMUNICATION
Journal Name
Initially, HepG2 cells with or without pretreatment by to significant drug accumulation in HepG2 cancer cells. This
galactose were incubated with GalP5 prodrug nanoparticles study paves an alternative way to construct supramolecular
⊃
for 1 h and 4 h, respectively. As shown in Fig. 5, the blue targeting prodrug nanoparticles with stimuli-responsiveness,
G
fluorescence of CPT could be detected after 1h incubation, which have great potential applications in the fields of
demonstrating that GalP5
successfully internalized by HepG2 cells. Upon extending the
incubation time to h, HepG2 cells showed intense Program of China (2014CB846004) and National Natural
⊃
G
prodrug nanoparticles were targeted drug delivery.
This work was supported by the National Basic Research
4
intracellular blue fluorescence, indicating the efficient Science Foundation of China (No. 21572101, 21472089).
intracellular CPT accumulation with extended culture time.
Furthermore, strong purple fluorescence that overlapped with
Notes and references
the lysosome-labeled fluorescence was observed, suggesting
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lysosomes. In contrast, HepG2 cells that were preincubated
with free galactose showed very weak intracellular CPT
fluorescence after 1 h and even 4 h incubation. Based on the
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⊃
G
prodrug
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expressed HepG2 cells via receptor-mediated endocytosis, and
then efficiently released anticancer drug to kill cancer cells.
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Fig. 5 CLSM images: (a) HepG2 cells incubated with GalP5⊃G
prodrug nanoparticles (10 μM) for 1 h and 4 h, respectively; (b)
HepG2 cells pretreated with free galactose for 15 min and then
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soluble pillar[5]arene (GalP5) and a CPT-based prodrug (
G).
9
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G
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7,
stable supramolecular nanoparticles under physiological
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3
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further revealed that GalP5⊃G prodrug nanoparticles could be
selectively recognized by HepG2 cells and then efficiently kill
cancer cells via receptor-mediated endocytosis, thus the side
effects to normal cells were remarkably reduced. Significantly,
CLSM experiments proved that these nanoparticles could lead
4 | Chem. Commun., 2017, 00, 1-3
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