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Mitochondria-Targeted Photoactivatable Real-Time Monitoring of a Controlled Drug Delivery Platform
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-12-10 , DOI: 10.1021/acs.jmedchem.1c00956 Neelu Singh 1 , Ajay Gupta 1 , Puja Prasad 2 , Raj Kumar Sah 3 , Arvind Singh 4 , Sunil Kumar 4 , Shailja Singh 3 , Shalini Gupta 2 , Pijus K Sasmal 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-12-10 , DOI: 10.1021/acs.jmedchem.1c00956 Neelu Singh 1 , Ajay Gupta 1 , Puja Prasad 2 , Raj Kumar Sah 3 , Arvind Singh 4 , Sunil Kumar 4 , Shailja Singh 3 , Shalini Gupta 2 , Pijus K Sasmal 1
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The current anticancer therapies are limited by their lack of controlled spatiotemporal release at the target site of action. We report a novel drug delivery platform that provides on-demand, real-time, organelle-specific drug release and monitoring upon photoactivation. The system is comprised of a model anticancer drug doxorubicin, an alkyltriphenylphosphonium moiety to target mitochondria in cancer cells, and a hydroxycinnamate photoactivatable linker that is covalently attached to the drug and mitochondria-targeting moieties such that it can be phototriggered by either UV (one-photon) or NIR (two-photon) light to form a fluorescent coumarin product and facilitate the release of drug payload. The extent of drug release is quantified by the fluorescence intensity of the coumarin formed. Further, the photoactivatable prodrug accumulates in the mitochondria and shows light-triggered temporally controlled cell death. In the future, our platform can be tuned for any biological application of interest, offering immense value in biomedicine.
中文翻译：
受控药物输送平台的线粒体靶向光激活实时监测
目前的抗癌疗法受限于它们在作用靶点缺乏受控的时空释放。我们报告了一种新型药物递送平台，该平台可提供按需、实时、细胞器特异性药物释放和光活化监测。该系统由模型抗癌药物多柔比星、靶向癌细胞线粒体的烷基三苯基鏻部分和共价连接到药物和线粒体靶向部分的羟基肉桂酸酯光激活接头组成，这样它就可以被紫外线（一种光子）或 NIR（双光子）光形成荧光香豆素产物并促进药物有效载荷的释放。药物释放的程度通过所形成的香豆素的荧光强度来量化。更远，可光激活的前药在线粒体中积累并显示光触发的时间控制细胞死亡。将来，我们的平台可以针对任何感兴趣的生物应用进行调整，在生物医学中提供巨大的价值。
更新日期：2021-12-23
中文翻译：
受控药物输送平台的线粒体靶向光激活实时监测
目前的抗癌疗法受限于它们在作用靶点缺乏受控的时空释放。我们报告了一种新型药物递送平台，该平台可提供按需、实时、细胞器特异性药物释放和光活化监测。该系统由模型抗癌药物多柔比星、靶向癌细胞线粒体的烷基三苯基鏻部分和共价连接到药物和线粒体靶向部分的羟基肉桂酸酯光激活接头组成，这样它就可以被紫外线（一种光子）或 NIR（双光子）光形成荧光香豆素产物并促进药物有效载荷的释放。药物释放的程度通过所形成的香豆素的荧光强度来量化。更远，可光激活的前药在线粒体中积累并显示光触发的时间控制细胞死亡。将来，我们的平台可以针对任何感兴趣的生物应用进行调整，在生物医学中提供巨大的价值。
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