Goldenseal (Hydrastis canadensis)
Effects of Herbal Products and their Constituents on Human Cytochrome P4502E1 Activity
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Ethanolic extracts from fresh Echinacea purpurea and Spilanthes acmella and dried Hydrastis canadensis were examined with regard to their ability to inhibit cytochrome P4502E1 mediated oxidation of p-nitrophenol in vitro. In addition, individual constituents of these extracts, including alkylamides from E. purpurea and S. acmella, caffeic acid derivatives from E. purpurea, and several of the major alkaloids from H. canadensis, were tested for inhibition using the same assay. H. canadensis (goldenseal) was a strong inhibitor of the P4502E1, and the inhibition appeared to be related to the presence of the alkaloids berberine, hydrastine and canadine in the extract. These compounds inhibited 2E1 with KI values ranging from 2.8 μM for hydrastine to 18 μM for berberine. The alkylamides present in E. purpurea and S. acmella also showed significant inhibition at concentrations as low as 25 μM, whereas the caffeic acid derivatives had no effect. Commercial green tea preparations, along with four of the individual tea catechins, were also examined and were found to have no effect on the activity of P4502E1.
1 . CYP2E1 Inhibition by Berberine (id=NPDI-Wkqo4w)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used — not specified
- CYP2E1 4173608
Cell fraction Pooled human liver microsomes -7999662
Results
Table 3
n and significance not indicated
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.5 mL
NADPH
0.020 mM
20 min
NADPH with precipitant
4.0 μM
2 . CYP2E1 Inhibition by GS root extract (id=NPDI-jjfDSA)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used — not specified
- CYP2E1 4173608
Cell fraction Pooled human liver microsomes -7999662
Results
Table 3 - n is not indicated
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.5 mL
NADPH
0.020 mM
20 min
NADPH with precipitant
3 . 2E1 Inhibition by Hydrastine (id=NPDI-aGqWbw)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used — not specified
- CYP2E1 4173608
Cell fraction Pooled human liver microsomes -7999662
"hydrastine being most potent [inhibitor]"
Results
Table 3
n and significance not indicated
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.5 mL
NADPH
0.020 mM
20 min
NADPH with precipitant
4.0 μM