Fluorescent Coumarin–Artemisinin Conjugates as Mitochondria‐Targeting Theranostic Probes for Enhanced Anticancer Activities |
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| Authors: | Dr Xu Zhang Qian Ba Zhanni Gu Dr Diliang Guo Prof Yu Zhou Prof Yungen Xu Prof Hui Wang Prof Deju Ye Prof Hong Liu |
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| Affiliation: | 1. CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203 (P.R. China);2. Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009 (P.R. China);3. Key Laboratory of Food Safety Research, Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai (P.R. China);4. Key Laboratory of Food Safety Risk Assessment, Ministry of Health, Beijing (P.R. China);5. State Key Laboratory of Analytical Chemistry for Life Science, and Collaborative Innovation Center of Chemistry for, Life Sciences School of Chemistry and Chemical Engineering, Nanjing University, 22 Hankou Road, Nanjing 210093 (P.R. China) |
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| Abstract: | 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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| Keywords: | apoptosis cancer drug delivery imaging agents theranostic probes |
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