Coptis (Coptis chinensis)
Coptis rhizome extract Nuclear Receptor Induction study - Ole Miss
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PXR is a key regulator for the expression of CYP 3A4 which is involved in the metabolism of majority of clinical drugs. Induction of PXR has been known to be associated with pharmacokinetic drug interactions.
AhR is involved in regulation of the expression of certain CYP isoforms. Phytochemicals could be the AhR agonists and induction of AhR could play a role in herb-drug interation.
1 . Coptis - In Vitro Nuclear Receptor Induction PXR Experiment - 2 (id=NPDI-yNQWkw)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Pregnane X receptor (PXR)
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
50,000 cells/well in 96-well plates
No
20 µg/mL
24 hrs for PXR induction
2 . Coptis - In Vitro Nuclear Receptor Induction AHR Experiment - 1 (id=NPDI-eSAGAA)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Aryl hydrocarbon receptor (AHR)
Cell system AhR reporter cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
200 µL of the proprietary cells / well provided with the AhR assay kit (Indigo Bioscience)
No
30 µg/mL
24 hrs for AhR inducing activity
3 . Coptis - In Vitro Nuclear Receptor Induction AHR Experiment - 2 (id=NPDI-UeS5mg)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Aryl hydrocarbon receptor (AHR)
Cell system AhR reporter cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
200 µL of the proprietary cells / well provided with the AhR assay kit (Indigo Bioscience)
No
10 µg/mL
24 hrs for AhR inducing activity
4 . Coptis - In Vitro Nuclear Receptor Induction PXR Experiment - 1 (id=NPDI-vv6jIQ)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Pregnane X receptor (PXR)
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
50,000 cells/well in 96-well plates
No
60 µg/mL
24 hrs for PXR induction
5 . Coptis - In Vitro Nuclear Receptor Induction AHR Experiment - 3 (id=NPDI-9ybaNw)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Aryl hydrocarbon receptor (AHR)
Cell system AhR reporter cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
200 µL of the proprietary cells / well provided with the AhR assay kit (Indigo Bioscience)
No
3.3 µg/mL
24 hrs for AhR inducing activity
6 . Coptis - In Vitro Nuclear Receptor Induction PXR Experiment - 3 (id=NPDI-rYnPHw)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
An activation of 2-folds or higher.
- Pregnane X receptor (PXR)
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
Luciferase activity (Reporter gene assay)
50,000 cells/well in 96-well plates
No
6.7 µg/mL
24 hrs for PXR induction