- Natural product: Kratom (Mitragyna speciosa)
- Associated study: Inhibitory effect of mitragynine on human cytochrome P450 enzyme activities
In Vitro Enzyme Inhibition Experiment
POS. CONTROL: Inhibition of CYP3A4 by ketoconazole
Inhibition was detected. Cutoff used — High probability of interaction if their IC50 values are less than 1 µM. If IC50 values are between 1 and 10 µM, they have moderate possibility in interaction. Low drug-drug interactions if their IC50 values are greater than 10 µM.
- CYP3A4 4306811
Recombinant expression system Baculovirus-insect cells
Cytochrome B5 Co-expressed
Positive control
Results
Positive control
IC50 values from Table 1
% enzyme inhibition versus precipitant concentration:
Values estimated from Figure 2. In some cases, SEM could not be estimated from the provided figure.
0.02 μM: 37 ± Unknown%
0.2 μM: 71 ± 3%
2 μM: 77 ± Unknown%
20 μM: 89 ± 7%
200 μM: See above data
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Positive inhibitors which are sulfaphenazole, quinidine and ketoconazole were purchased from Sigma Chemicals (St. Louis, USA). This assay was carried out using the P450-Glo™ Screening Systems from Promega, USA.
Positive control
Commercially available
50 min
NADPH regenerating system
Not available
Not available
0.02-200 µM