The individual or combinational effects of Hesperetin and Letrozole on the activity and expression of aromatase in MCF-7 cells.
Aromatase catalyzes the last and rate-limiting step in estrogen biosynthesis. Inhibition of estrogen production is a common strategy for breast cancer treatment. Citrus flavonoids have been confirmed to exhibit efficacious biological activities, particularly in cancer therapy. This study was carried out to investigate the effect of hesperetin on the activity and expression of aromatase and compare this property with letrozole as an aromatase inhibitor in MCF-7 breast cancer cell line. 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide (MTT) assays in this study demonstrated that hesperetin at a concentration of 200 μM decreased cell viability in a time dependent manner (P<0.05). Aromatase activity assay, based on 17β-Estradiol (E2) production from testosterone, revealed that hesperetin had no effect. Real-time PCR results indicated that treatment with 1μM concentration of hesperetin for 48 h significantly decreased relative aromatase expression (P =0.004). Combination of letrozole and hesperetin also had no effect on aromatase. The changes in activity paralleled the expression of aromatase. Likely, the reduction in aromatase activity was delayed in time along with the reduction in expression ratio; however additional studies are needed to confirm this. In conclusion, the present study showed that hesperetin could decrease expression of aromatase at low concentrations in MCF-7 breast cancer cells.
Iran University of Medical Sciences Department of Nutrition, School of Public Health Tehran Iran.
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Rahideh
Iran University of Medical Sciences Department of Nutrition, School of Public Health Tehran Iran.
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Shidfar
Iran University of Medical Sciences Department of Biochemistry, School of Medicine Tehran Iran.
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Nourbakhsh
Tehran University of Medical Sciences Department of Epidemiology and Biostatistics, School of Public Health Tehran Iran.
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Hoseini
Tehran University of Medical Sciences Department of Molecular and Cellular Nutrition, School of Nutritional Sciences and Dietetics Tehran Iran.
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Koohdani
Tehran University of Medical Sciences Department of Medical Genetics, School of Medicine Tehran Iran.
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Entezam
Tehran University of Medical Sciences Department of Medical Genetics, School of Medicine Tehran Iran keramatipour@sina.tums.ac.ir.
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Keramatipour
D001141:Aromatase / Q000235:genetics / Q000378:metabolism*; D002470:Cell Survival / Q000187:drug effects; D057075:Enzyme Assays; D004958:Estradiol / Q000378:metabolism; D006569:Hesperidin / Q000494:pharmacology*; D006801:Humans; D000077289:Letrozole; D061986:MCF-7 Cells; D009570:Nitriles / Q000494:pharmacology*; D060888:Real-Time Polymerase Chain Reaction; D014230:Triazoles / Q000494:pharmacology*
D009570:Nitriles; D014230:Triazoles; D004958:Estradiol; D000077289:Letrozole; D006569:Hesperidin; D001141:Aromatase; C013015:hesperetin