3A4/5 Inhibition by Goldenseal CSV JSON

In Vitro Enzyme Inhibition Experiment

3A4/5 Inhibition by Goldenseal

Inhibition was detected.  Cutoff used — not specified

midazolam 708298

1'-hydroxymidazolam

  • CYP3A

Cell fraction Pooled human liver microsomes -7999662

Results

Figure 2.

After incubation with the serum samples G1, G2, G3, G4,G5 (30, 100, 300, 600, 1000 μM) the activity of CYP3A on midazolam 1’-hydroxylation was determined to be 100.8±2.7%, 103.0±3.1%, 90.0±3.1%, 84.8±1.7%, 87.5%±2.3% of the control, respectively.

Compared to the control, G3, G4 and G5 significantly inhibited CYP3A4/5 activity (Figure 2). Interestingly, these three samples contained relatively higher concentrations of hydrastine (2.19-22.90-fold) than those in the samples G1 and G2 while berberine concentrations in the samples G3, G4, and G5 were lower (0.08-0.17 folds) than those in samples G1 and G2. In general, subjects administered GS exhibited higher hydrastine serum concentrations than berberine

Compound measured Measurement Value Study sequence Additional information N replicates

Experimental Conditions

0.2 mg/ml

80 μl

10 min

NADPH regenerating system

10 μM

10 min

30, 100, 300, 600, 1000 μM