Figure 1
Effect of bergamottin on testosterone CYP3A4 activity in human hepatocytes.
A, cultured human hepatocytes were treated with 0, 0.1, 1, 5, and 25 μM bergamottin along with 200 μM testosterone for 30 min. B, hepatocytes from a different donor were pretreated for 48 h with 10 μM rifampicin. At the end of 48 h, the culture medium was discarded, and fresh medium containing indicated concentrations of beragmottin or TAO (μM) and 200 μM testosterone was added to the cells (B). TAO was added 1 h before bergamottin. After 30 min of incubation, aliquots of medium were taken, and 6β-hydroxytestosterone was measured by HPLC as described under Materials and Methods. Each value represents the mean of duplicate treatments with the range indicated by the vertical bars. UN, control cells; n.d., not detected; Ber, bergamottin; Rif, rifampicin.