Diosmetin is a natural O-methylated flavone that is structurally related to luteolin . It reversibly inhibits cytochrome P450 (CYP) isoforms 1A1 and 1B1 in human liver microsomes with Ki values of 89 and 16 nM, respectively. It less potently inhibits CYP2C8 and CYP2C9 (Kis = 3.1 and 1.7 μM, respectively). While diosmetin inhibits CYP1A1 activity, it increases the transcription of the CYP1A1 gene in MCF-7 cells by activating the aryl hydrocarbon receptor when applied at 5 μM. Diosmetin also inhibits signaling through the stem cell factor receptor, c-Kit, at micromolar concentrations.
