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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

(a) Fluorescence imaging of Mito Tracker Red (0.5 μM, λem=598 nm) in SGC-7901 cells. (b) Fluorescence imaging of FPB (0.5 μM, λem = 514 nm) in SGC-7901 cells. (c) Overlapped image of (a) and (b). (d) Flow cytometry analysis of FPB uptake content in SGC-7901 cells and GES-1 cells.
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f4: (a) Fluorescence imaging of Mito Tracker Red (0.5 μM, λem=598 nm) in SGC-7901 cells. (b) Fluorescence imaging of FPB (0.5 μM, λem = 514 nm) in SGC-7901 cells. (c) Overlapped image of (a) and (b). (d) Flow cytometry analysis of FPB uptake content in SGC-7901 cells and GES-1 cells.

Mentions: To access the intracellular distribution of FPB in SGC-7901 cells, we performed a colocalization experiment using Nikon A1 Confocal laser scanning microscope. The cells were first incubated with FPB in the culture medium for 24 h, and then stained with Mito Tracker Red, a commercial mitochondrial dye. Figure 4b directly suggested that FPB display intriguing fluorescent property in SGC-7901 cells and could be directly visualized in living cells. From a contrasting merged image of FPB and Mito Tracker Red staining, we can observe that the FPB fluorescence perfectly overlapped with the mitochondria staining (Fig. 4c), which indicated that the mitochondria were the major concentrating organelle of FPB in the cell. Moreover, the optical properties of FPB were investigated in aqueous solution (Fig. S3 (SI)). FPB exhibits strong and narrow emission at 514 nm (full-width at half-maximum = 30 nm) and the fluorescence quantum yield is 20.2% (using fluorescein in ethanol as the reference). The remarkable optical properties allowed the direct visualization of FPB in cells. The results strongly demonstrate the excellent mitochondrial targeting and subcellular imaging capability of FPB in living carcinoma cells.


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)

(a) Fluorescence imaging of Mito Tracker Red (0.5 μM, λem=598 nm) in SGC-7901 cells. (b) Fluorescence imaging of FPB (0.5 μM, λem = 514 nm) in SGC-7901 cells. (c) Overlapped image of (a) and (b). (d) Flow cytometry analysis of FPB uptake content in SGC-7901 cells and GES-1 cells.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f4: (a) Fluorescence imaging of Mito Tracker Red (0.5 μM, λem=598 nm) in SGC-7901 cells. (b) Fluorescence imaging of FPB (0.5 μM, λem = 514 nm) in SGC-7901 cells. (c) Overlapped image of (a) and (b). (d) Flow cytometry analysis of FPB uptake content in SGC-7901 cells and GES-1 cells.
Mentions: To access the intracellular distribution of FPB in SGC-7901 cells, we performed a colocalization experiment using Nikon A1 Confocal laser scanning microscope. The cells were first incubated with FPB in the culture medium for 24 h, and then stained with Mito Tracker Red, a commercial mitochondrial dye. Figure 4b directly suggested that FPB display intriguing fluorescent property in SGC-7901 cells and could be directly visualized in living cells. From a contrasting merged image of FPB and Mito Tracker Red staining, we can observe that the FPB fluorescence perfectly overlapped with the mitochondria staining (Fig. 4c), which indicated that the mitochondria were the major concentrating organelle of FPB in the cell. Moreover, the optical properties of FPB were investigated in aqueous solution (Fig. S3 (SI)). FPB exhibits strong and narrow emission at 514 nm (full-width at half-maximum = 30 nm) and the fluorescence quantum yield is 20.2% (using fluorescein in ethanol as the reference). The remarkable optical properties allowed the direct visualization of FPB in cells. The results strongly demonstrate the excellent mitochondrial targeting and subcellular imaging capability of FPB in living carcinoma cells.

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