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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

Effects of FPB on mitochondrial membrane potential and ROS level.(a) Mitochondrial membrane potential is reflected as mean fluorescence intensity of TMRM determined by flow cytometry. (b) Flow cytometry analysis of ethidium bromide-DNA fluorescence resulting from DHE oxidation as a measure of ROS levels. Data are presented as the mean ± SD of three independent experiments.
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f6: Effects of FPB on mitochondrial membrane potential and ROS level.(a) Mitochondrial membrane potential is reflected as mean fluorescence intensity of TMRM determined by flow cytometry. (b) Flow cytometry analysis of ethidium bromide-DNA fluorescence resulting from DHE oxidation as a measure of ROS levels. Data are presented as the mean ± SD of three independent experiments.

Mentions: Next, we analysed physiological alterations of mitochondria in cancer cells treated by FPB. A decrease in ΔΨm is a hallmark of cells that precede apoptosis through the mitochondria insults33. The dissipation of ΔΨm could be detected by the fluorescent probe tetramethylrhodamine methyl ester (TMRM) which accumulates in the mitochondrial matrix in proportion to ΔΨm34. A representative flow cytometric plot reflecting the effect of FPB on SGC-7901 cells after incubation for 48 h is shown in Fig. S7 and mean fluorescence intensity of TMRM was reflected in Fig. 6a. As shown in Fig. 6a, treatment of SGC-7901 cells with FPB could induce dissipation of ΔΨm in a dose-dependent manner. As apoptosis is often accompanied by a decrease in ΔΨm, this result further confirms that FPB could induce cell apoptosis.


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)

Effects of FPB on mitochondrial membrane potential and ROS level.(a) Mitochondrial membrane potential is reflected as mean fluorescence intensity of TMRM determined by flow cytometry. (b) Flow cytometry analysis of ethidium bromide-DNA fluorescence resulting from DHE oxidation as a measure of ROS levels. Data are presented as the mean ± SD of three independent experiments.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f6: Effects of FPB on mitochondrial membrane potential and ROS level.(a) Mitochondrial membrane potential is reflected as mean fluorescence intensity of TMRM determined by flow cytometry. (b) Flow cytometry analysis of ethidium bromide-DNA fluorescence resulting from DHE oxidation as a measure of ROS levels. Data are presented as the mean ± SD of three independent experiments.
Mentions: Next, we analysed physiological alterations of mitochondria in cancer cells treated by FPB. A decrease in ΔΨm is a hallmark of cells that precede apoptosis through the mitochondria insults33. The dissipation of ΔΨm could be detected by the fluorescent probe tetramethylrhodamine methyl ester (TMRM) which accumulates in the mitochondrial matrix in proportion to ΔΨm34. A representative flow cytometric plot reflecting the effect of FPB on SGC-7901 cells after incubation for 48 h is shown in Fig. S7 and mean fluorescence intensity of TMRM was reflected in Fig. 6a. As shown in Fig. 6a, treatment of SGC-7901 cells with FPB could induce dissipation of ΔΨm in a dose-dependent manner. As apoptosis is often accompanied by a decrease in ΔΨm, this result further confirms that FPB could induce cell apoptosis.

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