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Fluorescent Coumarin-Artemisinin Conjugates as Mitochondria-Targeting Theranostic Probes for Enhanced Anticancer Activities.
Zhang, Xu; Ba, Qian; Gu, Zhanni; Guo, Diliang; Zhou, Yu; Xu, Yungen; Wang, Hui; Ye, Deju; Liu, Hong.
Afiliación
  • Zhang X; CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203 (P.R. China).
  • Ba Q; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009 (P.R. China).
  • Gu Z; Key Laboratory of Food Safety Research, Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai (P.R. China).
  • Guo D; Key Laboratory of Food Safety Risk Assessment, Ministry of Health, Beijing (P.R. China).
  • Zhou Y; CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203 (P.R. China).
  • Xu Y; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009 (P.R. China).
  • Wang H; CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203 (P.R. China).
  • Ye D; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009 (P.R. China).
  • Liu H; CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203 (P.R. China).
Chemistry ; 21(48): 17415-21, 2015 Nov 23.
Article en En | MEDLINE | ID: mdl-26458147
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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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cumarinas / Artemisininas / Colorantes Fluorescentes / Mitocondrias / Neoplasias Límite: Humans Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2015 Tipo del documento: Article Pais de publicación: Alemania

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Cumarinas / Artemisininas / Colorantes Fluorescentes / Mitocondrias / Neoplasias Límite: Humans Idioma: En Revista: Chemistry Asunto de la revista: QUIMICA Año: 2015 Tipo del documento: Article Pais de publicación: Alemania