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Fluorescent Coumarin–Artemisinin Conjugates as Mitochondria‐Targeting Theranostic Probes for Enhanced Anticancer Activities
Author(s) -
Zhang Xu,
Ba Qian,
Gu Zhanni,
Guo Diliang,
Zhou Yu,
Xu Yungen,
Wang Hui,
Ye Deju,
Liu Hong
Publication year - 2015
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201502543
Subject(s) - artemisinin , mitochondrion , cytotoxicity , coumarin , cancer cell , apoptosis , reactive oxygen species , intracellular , conjugate , chemistry , microbiology and biotechnology , pharmacology , biochemistry , cancer , cancer research , biology , in vitro , immunology , plasmodium falciparum , mathematical analysis , genetics , mathematics , organic chemistry , malaria
Mitochondria‐targeting theranostic probes that enable the simultaneously reporting of and triggering of mitochondrial dysfunctions in cancer cells are highly attractive for cancer diagnosis and therapy. Three fluorescent mitochondria‐targeting theranostic probes have been developed by linking a mitochondrial dye, coumarin‐3‐carboximide, with a widely used traditional Chinese medicine, artemisinin, to kill cancer cells. Fluorescence images showed that the designed coumarin–artemisinin conjugates localized mainly in mitochondria, leading to enhanced anticancer activities over artemisinin. High cytotoxicity against cancer cells correlated with the strong ability to accumulate in mitochondria, which could efficiently increase the intracellular reactive oxygen species level and induce cell apoptosis. This study highlights the potential of using mitochondria‐targeting fluorophores to selectively trigger and directly visualize subcellular drug delivery in living cells.