TABLE 3

Inhibition of the 7-ethoxyresorufin O-deethylation activity of CYP1 by demethyleneberberine, thalifendine, and berberrubine

Inhibition of CYP1-catalyzed 7-ethoxyresorufin O-deethylation activity was studied in the assays without NADPH-fortified preincubation. IC50 value was calculated, as described in Materials and Methods. Data show the estimates and estimates of variance (denoted by ±) determined from the curve fit analysis of individual sets of data.

P450IC50, μM
DemethyleneberberineThalifendineBerberrubine
CYP1A1>6030.4 ± 1.2>60
CYP1A2>60>60>60
CYP1B1.18.0 ± 1.210.0 ± 0.926.7 ± 1.4