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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 and F16 on cell proliferation (5 days) at different concentrations.Black, effect of FPB on SGC-7901 cells proliferation. Red, effect of F16 on SGC-7901 cells proliferation. Blue, effect of FPB on NIH/3T3 cells proliferation. Cyan, effect of F16 on NIH/3T3 cells proliferation. Data are presented as the mean ± SD of two independent experiments.
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f3: Effects of FPB and F16 on cell proliferation (5 days) at different concentrations.Black, effect of FPB on SGC-7901 cells proliferation. Red, effect of F16 on SGC-7901 cells proliferation. Blue, effect of FPB on NIH/3T3 cells proliferation. Cyan, effect of F16 on NIH/3T3 cells proliferation. Data are presented as the mean ± SD of two independent experiments.

Mentions: Information on cell proliferation is one of the most the important indicators in the evaluation of drug effect and physiological research. The MTT cell proliferation assay has already been demonstrated to be a rapid, versatile, quantitative, and highly reproducible colorimetric assay for determining viable cell number in proliferation2829. The effects of FPB on cell proliferation were measured by MTT cell proliferation assay using SGC-7901 cells and 3T3 cells. The effect of F16 was also studied for comparison. As shown in Fig. 3, the proliferation of SGC-7901 cells was significantly inhibited by 2 μM FPB or F16 upon 5 days of exposure while 3T3 cells proliferation was not affected under the same conditions. Compared with F16, FPB shows a little weaker efficiency on inhibition of cancer cell proliferation at low concentration. At a concentration of 2 μM, the difference is approximately 10%. Based on these results, we can conclude that FPB has a similar selectivity and anti-proliferative activity as F16.


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 and F16 on cell proliferation (5 days) at different concentrations.Black, effect of FPB on SGC-7901 cells proliferation. Red, effect of F16 on SGC-7901 cells proliferation. Blue, effect of FPB on NIH/3T3 cells proliferation. Cyan, effect of F16 on NIH/3T3 cells proliferation. Data are presented as the mean ± SD of two independent experiments.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f3: Effects of FPB and F16 on cell proliferation (5 days) at different concentrations.Black, effect of FPB on SGC-7901 cells proliferation. Red, effect of F16 on SGC-7901 cells proliferation. Blue, effect of FPB on NIH/3T3 cells proliferation. Cyan, effect of F16 on NIH/3T3 cells proliferation. Data are presented as the mean ± SD of two independent experiments.
Mentions: Information on cell proliferation is one of the most the important indicators in the evaluation of drug effect and physiological research. The MTT cell proliferation assay has already been demonstrated to be a rapid, versatile, quantitative, and highly reproducible colorimetric assay for determining viable cell number in proliferation2829. The effects of FPB on cell proliferation were measured by MTT cell proliferation assay using SGC-7901 cells and 3T3 cells. The effect of F16 was also studied for comparison. As shown in Fig. 3, the proliferation of SGC-7901 cells was significantly inhibited by 2 μM FPB or F16 upon 5 days of exposure while 3T3 cells proliferation was not affected under the same conditions. Compared with F16, FPB shows a little weaker efficiency on inhibition of cancer cell proliferation at low concentration. At a concentration of 2 μM, the difference is approximately 10%. Based on these results, we can conclude that FPB has a similar selectivity and anti-proliferative activity as F16.

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