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ChemComm
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Fig. 6 The anti-tumour effect of Epi-GA in HepG2-inoculated xenograft
models. (a) HepG2 cells were injected into athymic nu/nu mice and grown
for 6 days before the first i.p. administration of Epi and Epi-GA (arrowhead).
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1 mg Epi and Epi-GA per kg body weight per injection]. Tumour size is
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(b) After 28 days, the HepG2-driven tumour tissues were removed, weighed
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In conclusion, we have reported a glycyrrhetinic acid
(GA)-decorated fluorescent probe, Cou-GA, to evaluate the liver
cancer targeting ability of GA using a small organic molecule based
approach. Our in vitro results confirmed that GA-modification
enhances the cellular uptake of the fluorescent probe Cou-GA into
hepatocellular carcinoma (HCC). Furthermore, the potential of GA
as an active HCC targeting unit with prodrug, Epi-GA, was also
proved. Notably, Epi-GA was found to display selective cytotoxicity
towards HepG2 and Chang liver cells due to preferential
cellular uptake followed by self-immolative release of active
drug (Epi) by elevated esterase enzyme activity in the cells.
Collectively, these results prove GA as an alternative choice for
developing new small molecule based targeted diagnostic and
therapeutic methods for HCC.
This work was supported by CRI (Grant No. 2009-0081566
and 2018R1A3B1052702, J. S. K.) and NRF (Grant No.
2017R1A2A2A05069805, C. K., and 2014R1A6A3A04058006,
D. H. K.) of Korea.
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Conflicts of interest
There are no conflicts to declare.
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12356 | Chem. Commun., 2018, 54, 12353--12356
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