- Natural product: Goldenseal (Hydrastis canadensis)
- Associated study: An ex vivo approach to botanical-drug interactions: A proof of concept study
In Vitro Enzyme Inhibition Experiment
3A4/5 Inhibition by Goldenseal
Inhibition was detected. Cutoff used — not specified
- 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
| Sample | Compound measured | Value | Measurement | 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