Abstract
Mitochondria have recently emerged as novel targets for cancer therapy due to its important roles in fundamental cellular function. Discovery of new chemotherapeutic agents that allow for simultaneous treatment and visualization of cancer is urgent. Herein, we demonstrate a novel bifunctional mitochondria-targeted anticancer agent (FPB), exhibiting both imaging capability and anticancer activity. It can selectively accumulate in mitochondria and induce cell apoptosis. Notably, it results in much higher toxicity toward cancer cells owing to much higher uptake by cancer cells. These features make it highly attractive in cancer imaging and treatment.
Highlights
We report a novel bifunctional mitochondria-targeted anticancer agent FPB, by conjugating F16, a Delocalized lipophilic cations (DLCs) compound, and boron-dipyrromethene (BODIPY), a widely used fluorescent dye, with a phenylethynyl linker (Fig. 1)
A lot of attention has been drawn to mitochondria as potential targets of anticancer therapy because of their crucial involvement in cell death[2,3,10]
Driving by the mitochondrial membrane potential, FPB could accumulate in cancer cell mitochondrial and affect the function of mitochondria
Summary
We report a novel bifunctional mitochondria-targeted anticancer agent FPB, by conjugating F16, a DLC compound, and boron-dipyrromethene (BODIPY), a widely used fluorescent dye, with a phenylethynyl linker (Fig. 1). To the best of our knowledge, there are few reports on utilizing F16 as a cargo group to target mitochondria. Biological investigations suggest that FPB is a promising multifunctional anticancer agent that incorporates optical monitoring capability and selective anticancer activity. FPB could accumulate in carcinoma mitochondria and induce cell apoptosis. Our study suggested that F16 could be used as a mitochondria-targeted moiety to design anticancer drugs
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