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A novel bifunctional mitochondria-targeted anticancer agent with high selectivity for cancer cells.

He H, Li DW, Yang LY, Fu L, Zhu XJ, Wong WK, Jiang FL, Liu Y - Sci Rep (2015)

Bottom Line: 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.These features make it highly attractive in cancer imaging and treatment.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Virology &Key Laboratory of Analytical Chemistry for Biology and Medicine (MOE), College of Chemistry Molecular Sciences, Wuhan University, Wuhan 430072, P. R. China.

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.

No MeSH data available.


Related in: MedlinePlus

The synthetic route of FPB.
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f1: The synthetic route of FPB.

Mentions: We now 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. Moreover, our study suggested that F16 could also be used as a mitochondria-targeted moiety to design anticancer drugs.


A novel bifunctional mitochondria-targeted anticancer agent with high selectivity for cancer cells.

He H, Li DW, Yang LY, Fu L, Zhu XJ, Wong WK, Jiang FL, Liu Y - Sci Rep (2015)

The synthetic route of FPB.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4559806&req=5

f1: The synthetic route of FPB.
Mentions: We now 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. Moreover, our study suggested that F16 could also be used as a mitochondria-targeted moiety to design anticancer drugs.

Bottom Line: 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.These features make it highly attractive in cancer imaging and treatment.

View Article: PubMed Central - PubMed

Affiliation: State Key Laboratory of Virology &Key Laboratory of Analytical Chemistry for Biology and Medicine (MOE), College of Chemistry Molecular Sciences, Wuhan University, Wuhan 430072, P. R. China.

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.

No MeSH data available.


Related in: MedlinePlus