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首页> 外文期刊>Chemistry: A European journal >Designed Benzothiadiazole Fluorophores for Selective Mitochondrial Imaging and Dynamics
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Designed Benzothiadiazole Fluorophores for Selective Mitochondrial Imaging and Dynamics

机译：设计的苯并噻二唑荧光团用于线粒体选择性成像和动力学

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摘要

A series of new rationale designed 2,1,3-benzothiadiazole (BTD) fluorescent derivatives has been synthesized and applied for cellular selective staining of cancer cells in cell-imaging experiments. Four new synthesized BTD derivatives showed only poor or reasonable cellular selection, but with excellent fluorescence intensity and almost no background signal emitting at the blue or green channels. The knowledge gained by analysing their molecular architecture, however, allowed the planning and synthesis of a fluorescent BTD, which was then successfully tested and showed superior mitochondrial selection with outstanding results in bioimaging experiments in living cells. The new marker (named Splendor) was then compared with the commercially available MitoTracker Red (also through co-staining experiments) and showed far better mitochondrial selection, fluorescence intensity and chemical stability. Mitochondrial imaging and tracking (dynamic changes) was possible using Splendor during the whole cellular division cycle. DFT calculations were performed to offer insights into the origin of the chemical-and photostability of BTD derivatives. In addition, molecular docking calculations hint at a potential molecular target for the BTD derivatives in the mitochondrial protein adenine nucleotide translocase, which may explain the mitochondrial selectivity of Splendor versus the other four BTD derivatives.
机译：合成了一系列新的基本原理设计的2,1,3-苯并噻二唑（BTD）荧光衍生物，并将其用于细胞成像实验中的癌细胞的细胞选择性染色。四种新的合成BTD衍生物仅显示出较差或合理的细胞选择，但具有出色的荧光强度，几乎没有蓝色或绿色通道发射的背景信号。但是，通过分析其分子结构获得的知识使荧光BTD得以计划和合成，然后成功地对其进行了测试，并显示出优异的线粒体选择，在活细胞的生物成像实验中具有出色的结果。然后将新标记（命名为Splendor）与市售的MitoTracker Red（也通过共染色实验）进行了比较，显示出更好的线粒体选择，荧光强度和化学稳定性。在整个细胞分裂周期中使用Splendor可以进行线粒体成像和跟踪（动态变化）。进行DFT计算以提供对BTD衍生物化学和光稳定性的起源的见解。此外，分子对接计算暗示线粒体蛋白腺嘌呤核苷酸转位酶中BTD衍生物的潜在分子靶标，这可能解释了Splendor对其他四种BTD衍生物的线粒体选择性。

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