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Econazole Nitrate Induces Apoptosis in MCF-7 Cells via Mitochondrial and Caspase Pathways.

Sun J, Yu CH, Zhao XL, Wang Y, Jiang SG, Gong XF - Iran J Pharm Res (2014)

Bottom Line: In addition, western blot analysis showed that EN resulted in the decrease expression of procaspase-3, procaspase-9 and bcl-2.In conclusion, these findings suggest that EN may be an effective way for treating human breast cancer.The anti-tumor mechanisms of EN might involve mitochondrial and caspase pathways.

View Article: PubMed Central - PubMed

Affiliation: School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080 , PR China.

ABSTRACT
Econazole nitrate (EN), a synthetic compound, is now in use as a routine antifungal drug. EN was shown to have antitumor effect, the tumor cell killing mechanisms, however, remain unclear. In this research, the apoptosis-inducing effect of EN on MCF-7 cells was investigated. The results showed that EN inhibited the proliferation of MCF-7 cells in a time- and dose-dependent manner by MTT method and colony forming assay. MCF-7 cells treated with EN showed typical characteristics of apoptosis including the morphological changes and DNA fragmentation. Meanwhile, the loss of mitochondrial membrane potential was showed by flow cytometry. In addition, western blot analysis showed that EN resulted in the decrease expression of procaspase-3, procaspase-9 and bcl-2. In conclusion, these findings suggest that EN may be an effective way for treating human breast cancer. The anti-tumor mechanisms of EN might involve mitochondrial and caspase pathways.

No MeSH data available.


Related in: MedlinePlus

The chemical structure of econazole nitrate (EN).
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Figure 1: The chemical structure of econazole nitrate (EN).

Mentions: It is known that azole derivatives have been shown to exert anti-tumor effect (1-4). Econazole nitrate (EN) (Figure 1), one of imidazole anti-fungal agent (5-8), has been used in treatment of mycosis. EN has been shown to induce endoplasmic reticulum (ER) stress in HL-60 cells by promoting ER Ca2+ depletion and sustained protein synthesis inhibition (9-12) , suggesting that HL-60 cell is sensitive to EN. Meanwhile, EN increases the concentration of Ca2+ in MG63 osteosarcoma cells, which suggested that EN acts as a potent blocker of store-operated Ca2+ entry (13, 14). Furthermore, EN exerts inhibitory effect on the enzymes involved in the conversion of progesterone to testosterone in the H295R cell (15). Prostate cancer PC3 cells overnight treated with econazole (1-30 μΜ) resulted in decrease in cell proliferation by 20-100% (16). EN has also been shown to induce COLO 205 cells apoptosis by arrest cell cycle and caspases signaling pathways (17).


Econazole Nitrate Induces Apoptosis in MCF-7 Cells via Mitochondrial and Caspase Pathways.

Sun J, Yu CH, Zhao XL, Wang Y, Jiang SG, Gong XF - Iran J Pharm Res (2014)

The chemical structure of econazole nitrate (EN).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4232799&req=5

Figure 1: The chemical structure of econazole nitrate (EN).
Mentions: It is known that azole derivatives have been shown to exert anti-tumor effect (1-4). Econazole nitrate (EN) (Figure 1), one of imidazole anti-fungal agent (5-8), has been used in treatment of mycosis. EN has been shown to induce endoplasmic reticulum (ER) stress in HL-60 cells by promoting ER Ca2+ depletion and sustained protein synthesis inhibition (9-12) , suggesting that HL-60 cell is sensitive to EN. Meanwhile, EN increases the concentration of Ca2+ in MG63 osteosarcoma cells, which suggested that EN acts as a potent blocker of store-operated Ca2+ entry (13, 14). Furthermore, EN exerts inhibitory effect on the enzymes involved in the conversion of progesterone to testosterone in the H295R cell (15). Prostate cancer PC3 cells overnight treated with econazole (1-30 μΜ) resulted in decrease in cell proliferation by 20-100% (16). EN has also been shown to induce COLO 205 cells apoptosis by arrest cell cycle and caspases signaling pathways (17).

Bottom Line: In addition, western blot analysis showed that EN resulted in the decrease expression of procaspase-3, procaspase-9 and bcl-2.In conclusion, these findings suggest that EN may be an effective way for treating human breast cancer.The anti-tumor mechanisms of EN might involve mitochondrial and caspase pathways.

View Article: PubMed Central - PubMed

Affiliation: School of Chemistry and Materials Science, Heilongjiang University, Harbin 150080 , PR China.

ABSTRACT
Econazole nitrate (EN), a synthetic compound, is now in use as a routine antifungal drug. EN was shown to have antitumor effect, the tumor cell killing mechanisms, however, remain unclear. In this research, the apoptosis-inducing effect of EN on MCF-7 cells was investigated. The results showed that EN inhibited the proliferation of MCF-7 cells in a time- and dose-dependent manner by MTT method and colony forming assay. MCF-7 cells treated with EN showed typical characteristics of apoptosis including the morphological changes and DNA fragmentation. Meanwhile, the loss of mitochondrial membrane potential was showed by flow cytometry. In addition, western blot analysis showed that EN resulted in the decrease expression of procaspase-3, procaspase-9 and bcl-2. In conclusion, these findings suggest that EN may be an effective way for treating human breast cancer. The anti-tumor mechanisms of EN might involve mitochondrial and caspase pathways.

No MeSH data available.


Related in: MedlinePlus