Pyridinium and Indole Orientation Determines the Mitochondrial Uncoupling and Anti-Cancer Efficiency of F16

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  • 作者：Xu, J., He, H., Zhou, L. J., Liu, Y. Z., Li, D. W., Jiang, F. L. & Liu, Y.
  • 期刊：European journal of medicinal chemistry 154, 305-313 (2018)
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F16 is a mitochondria-targeted, broad-spectrum anticancer agent in the pre-clinic cancer therapy. Here we developed two fluorescent isomers of F16 (o-F16 and m-F16) with entirely different photophysical properties, uncoupling activity, and cytotoxicity by merely modifying the linking orientation of pyridinium and indole units. Individually, o-F16 acted as a strong uncoupler to reduce the mitochondrial respiration efficiency, while m-F16 could hardly uncouple the mitochondrial respiration due to its poor proton dissociation capability. Owing to their intrinsic fluorescence, o-F16 and m-F16 could specifically image mitochondria in the green and red channel, respectively. This work could provide useful information for the development of uncouplers and design of mitochondrial-targeted drugs.

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