Kratom (Mitragyna speciosa)
Exploration of cytochrome P450 inhibition mediated drug-drug interaction potential of kratom alkaloids
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In vitro cytochrome P450 inhibition of major kratom alkaloids: mitragynine (MTG), speciogynine (SPG), speciocilliatine (SPC), corynantheidine (COR), 7-hydroxymitragynine (7HMG) and paynantheine (PAY) was evaluated using human liver microsomes (HLMs) to understand their drug-drug interaction potential. CYP450 isoform- specific substrates of CYP1A2, 2C8, 2C9, 2C19, 2D6, and 3A4/5 were incubated in HLMs with or without alkaloids. Preliminary CYP450 inhibition (IC50) data were generated for each of these isoforms. In addition, the type of inhibition and estimation of the inhibition constants (Ki) of MTG and COR were determined. Among the tested alkaloids, MTG and COR were potent inhibitors of CYP2D6 (IC50, 2.2 and 4.2 μM, respectively). Both MTG and COR exhibited competitive inhibition of CYP2D6 activity and the Ki were found to be 1.1 and 2.8 μM, respectively. SPG and PAY showed moderate inhibition of CYP2D6 activity. Additionally, moderate inhibitory effects by SPC, MTG, and SPG were observed on CYP2C19 activity. Interestingly, inhibition of only midazolam hydroxylase CYP3A4/5 activity by COR, PAY, and MTG was observed while no inhibitory effect was observed when testosterone was used as a probe substrate. In conclusion, MTG and COR may lead to clinically significant adverse drug interactions upon coadministration of drugs that are substantially metabolized by CYP2D6.
1 . Inhibition of Mitragynine for CYP2C8 (id=NPDI-J2PdQQ)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
2 . Inhibition of Speciociliatine for CYP2C8 (id=NPDI-JqmF7w)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
3 . Inhibition of Corynantheidine for CYP2D6 (id=NPDI-qWS53g)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
4 . Inhibition of Mitragynine for CYP2D6 (id=NPDI-17YRkg)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
5 . Inhibition of Paynantheine for CYP2D6 (id=NPDI-K9DvIg)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
6 . Inhibition of Speciogynine for CYP2D6 (id=NPDI-Oq9KmA)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
7 . Inhibition of Corynantheidine for CYP2C9 (id=NPDI-bXPXRQ)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
1 - 100 µM
Control Experiment Information
8 . Inhibition of Paynantheine for CYP2C9 (id=NPDI-4HfEdA)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
0 - 100 µM
Control Experiment Information
9 . Inhibition of 7-hydroxymitragynine for CYP2C19 (id=NPDI-eMZPbA)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
1 - 100 µM
Control Experiment Information
10 . Inhibition of Mitragynine for CYP2C19 (id=NPDI-Ua1CeQ)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
Control Experiment Information
11 . Inhibition of Paynantheine for CYP2C19 (id=NPDI-wo-wRw)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
12 . Inhibition of Speciociliatine for CYP2C19 (id=NPDI-XQCOGw)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
13 . Inhibition of Speicogynine for CYP2C19 (id=NPDI-WIpfxQ)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
14 . Inhibition of Corynantheidine for CYP3A4/5 (id=NPDI-7PU97Q)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
1 - 100 µM
Control Experiment Information
15 . Inhibition of Mitragynine for CYP3A4/5 (id=NPDI-c_gPeA)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
1 - 100 µM
Control Experiment Information
16 . Inhibition of Paynantheine for CYP3A4/5 (id=NPDI-WakYGw)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
0 - 100 µM
Control Experiment Information
17 . Inhibition of Speciociliatine for CYP3A4/5 (id=NPDI-TTv3Iw)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
0 - 100 µM
Control Experiment Information
18 . Inhibition of Speciogynine for CYP3A4/5 (id=NPDI-QQeDSQ)
In Vitro Enzyme Inhibition Experiment
Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
0 - 100 µM
Control Experiment Information
19 . Weak Inhibition of 7-hydroxymitragynine for CYP2C8 (id=NPDI-U-ajPw)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
20 . Weak Inhibition of Corynantheidine for CYP2C8 (id=NPDI-o56vpA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
21 . Weak Inhibition of Paynantheine for CYP2C8 (id=NPDI-XeGihA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
22 . Weak Inhibition of Speciogynine for CYP2C8 (id=NPDI-B_7tOA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C8 4306333
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
23 . Weak Inhibition of 7-hydroxymitragynine for CYP2D6 (id=NPDI-cimaKA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
1 - 100 µM
Control Experiment Information
24 . Weak Inhibition of Speciociliatine for CYP2D6 (id=NPDI-ULP_qQ)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2D6 4173631
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
7 µM
0 - 100 µM
Control Experiment Information
25 . Weak Inhibition of 7-hydroxymitragynine for CYP2C9 (id=NPDI-DLH-JQ)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
1 - 100 µM
Control Experiment Information
26 . Weak Inhibition of Mitragynine for CYP2C9 (id=NPDI-0hNq0Q)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
0 - 100 µM
Control Experiment Information
27 . Weak Inhibition of Speciociliatine for CYP2C9 (id=NPDI-Zvn2gg)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
0 - 100 µM
Control Experiment Information
28 . Weak Inhibition of Speciogynine for CYP2C9 (id=NPDI-sN1pZA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C9 4309227
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
6 µM
0 - 100 µM
Control Experiment Information
29 . Weak Inhibition of Corynantheidine for CYP2C19 (id=NPDI-aGXuxA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP2C19 4311137
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
60 min
NADPH
40 µM
1 - 100 µM
Control Experiment Information
30 . Weak Inhibition of 7-hydroxymitragynine for CYP3A4/5 (id=NPDI-olaGPQ)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
10 min
NADPH
4 µM
1 - 100 µM
Control Experiment Information
31 . Weak Inhibition of 7-hydroxymitragynine for CYP1A2 (id=NPDI-1vxnrQ)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
1 - 100 µM
Control Experiment Information
32 . Weak Inhibition of Cornantheidine for CYP1A2 (id=NPDI-1Cjyxg)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
1 - 100 µM
Control Experiment Information
33 . Weak Inhibition of Mitragynine for CYP1A2 (id=NPDI-laH1lA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
34 . Weak Inhibition of Paynantheine for CYP1A2 (id=NPDI-V_oQog)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
35 . Weak Inhibition of Speciociliatine for CYP1A2 (id=NPDI-zKam8g)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
36 . Weak Inhibition of Speciogynine for CYP1A2 (id=NPDI-_MFsyA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP1A2 4312402
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 30 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
15 min
NADPH
40 µM
0 - 100 µM
Control Experiment Information
37 . Weak Inhibition of 7-hydroxymitragynine for CYP3A4/5 (id=NPDI-iASYyA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S4 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
1 - 100 µM
Control Experiment Information
38 . Weak Inhibition of Corynantheidine for CYP3A4/5 (id=NPDI-qMnZyA)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
1 - 100 µM
Control Experiment Information
39 . Weak Inhibition of Mitragynine for CYP3A4/5 (id=NPDI-BLzT_g)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure 2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
1 - 100 µM
Control Experiment Information
40 . Weak Inhibition of Paynantheine for CYP3A4/5 (id=NPDI-aNb3lw)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S5 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
0 - 100 µM
Control Experiment Information
41 . Weak Inhibition of Speciociliatine for CYP3A4/5 (id=NPDI-2seH4Q)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S3 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
0 - 100 µM
Control Experiment Information
42 . Weak Inhibition of Speciogynine for CYP3A4/5 (id=NPDI-P2Nw6g)
In Vitro Enzyme Inhibition Experiment
Negligible Inhibition was detected. Cutoff used —
IC50 = 45 μM
- CYP3A4 4306811
- CYP3A5
Cell fraction Pooled human liver microsomes -7999662
Results
% result estimated from Figure S2 at around 100 µM
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
0.1 mg/ml
200 µL
5 min
NADPH
100 µM
0 - 100 µM