Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 21, Issue 48, Pages 17415-17421Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201502543
Keywords
apoptosis; cancer; drug delivery; imaging agents; theranostic probes
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Funding
- National Natural Science Foundation of China [91229204, 81220108025, 21327902, 81125020]
- Major Project of Chinese National Programs for Fundamental Research and Development [2015C8910304]
- National High Technology Research and Development Program of China [2012AA020302]
- Science and Technology Commission of Shanghai Municipality [12431900500]
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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.
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