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Diosmetin (DIO) is an agonist of the aryl hydrocarbon receptor (AHR). It potently inhibited the enzyme activity of cytochrome P450 1A1 (CYP1A1) in a dose-dependent manner with an IC50 value of approximately 30 nM, in microsomes from MCF-7 cells [1].

AHR belongs to the Per, ARNT, Sim/basic-helix-loop-helix superfamily of ligand-activated transcription factors. AHR mediates the toxic effects of polycyclic aromatic hydrocarbons, 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and polychlorinated biphenyls. These chemicals all bind to AHR, and result in the activation of a battery of genes, including the cytochromes P450 CYP1A1, CYP1A2, and CYP1B1 [2].

In MCF-7 cells, at 24 h after the incubation of diosmetin, CYP1A1 mRNA was increased in a dose-dependent manner. In MCF-7 cells, diosmetin at 2.5 µM modestly increased CYP1A1 enzyme activity, with an activity increase in cells, while diosmetin at 5 µM did not increase the enzyme activity compared to controls in cells. Compared with controls, diosmetin dose-dependently increased the capacity of nuclear extracts to bind an oligonucleotide containing the AhR-binding sequence of CYP1A1 [1].

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