期刊
ADVANCED HEALTHCARE MATERIALS
卷 10, 期 21, 页码 -出版社
WILEY
DOI: 10.1002/adhm.202101144
关键词
drug-drug conjugates; fluorescent probes; prodrugs; synergistic therapy
资金
- National Natural Science Foundation of China [51873072, 52073101]
- Science and Technology Program of Guangzhou [202102010025]
- Guangdong Provincial Pearl River Talents Program [2019QN01Y088]
In this study, a theranostic heterodimeric prodrug, CyNH-SS-DOX, is developed for synergistic cancer therapy with dual-channel fluorescence monitoring of drug activation, enhancing therapeutic efficacy and minimizing side effects.
Theranostic prodrugs that can precisely monitor drug activation with synergistic therapeutic effects are highly desirable for personalized medicine. In this study, a theranostic heterodimeric prodrug, CyNH-SS-DOX, with synchronous and independent dual-channel fluorescence turn-on and dual-prodrug activation for synergistic cancer therapy is developed. A hemicyanine fluorescent drug, CyNH2, with good therapeutic effects found in this work, is conjugated to doxorubicin (DOX) through a disulfide linker to form CyNH-SS-DOX. Before activation, both the fluorescence of DOX and CyNH2 are in the off state and the toxicity is low. In the presence of intracellular glutathione, both the fluorescence of DOX and CyNH2 at different channels are turned on. Meanwhile, DOX and CyNH2 are activated in a synergistic anticancer effect. It is believed that CyNH-SS-DOX is promising for monitoring prodrug activation in dual-fluorescence channels and for enhancing therapeutic efficacy with few side effects.
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