Shrubby sophora (Sophora flavescens)
Chinese Herbal Medicine Sophora Flavescens Activates PXR
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Sophora Flavescens (SF) is widely used for treatment of viral hepatitis, cancer, viral myocarditis, gastrointestinal hemorrhage, and skin diseases. SF has been shown to up-regulate CYP3A expression, but this mechanism is not yet known. DPX2 and HepaRG were used to investigate the role of PXR in SF-induced CYP3A expression. A metabolomic approach was used to identify the chemical constituents in SF. N-methylcytisine, a chemical constituent, activated PXR and significantly induced CYP3A4 expression, which was suppressed by sulforaphane, a PXR antagonist. Thus, SF was shown to induce CYP3A expression via PXR activation.
1 . N-methylcytisine - Effect of Sophora Flavescens and N-Methylcytisine on CYP3A4 in DPX2 Cells Experiment - 1 (id=NPDI-3_AU-Q)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
2 . N-methylcytisine - Effect of Sophora Flavescens and N-Methylcytisine on CYP3A4 in HepaRG Cells Experiment - 1 (id=NPDI-DaTCfg)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
3 . N-methylcytisine - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 2 (id=NPDI-ITjgfQ)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
4 . N-methylcytisine - Effect on PXR Activation Experiment - 4 (id=NPDI-dIRh5Q)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
5 . Sophora Flavescens - Effect on PXR Activation in DPX2 Cells Experiment - 1 (id=NPDI-l6H7hA)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
≥ positive controls (Schisandrae chinensis Baill and Glycyrrhizae uralensis Fisch)
- 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)
480 mg/l
24 hours
6 . Sophora Flavescens - Effect of Sophora Flavescens 5 g/L and N-Methylcytisine on CYP3A4 in DPX2 Cells Experiment - 2 (id=NPDI-3jqrbg)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
5 g/L
48 hours
7 . Sophora Flavescens - Effect of Sophora Flavescens 1 g/L and N-Methylcytisine on CYP3A4 in DPX2 Cells Experiment - 3 (id=NPDI-DJBgHg)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
1 g/L
48 hours
8 . Sophora Flavescens - Effect of Sophora Flavescens 0.5 g/L and N-Methylcytisine on CYP3A4 in DPX2 Cells Experiment - 4 (id=NPDI-2Jtpug)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
0.5 g/L
48 hours
9 . Sophora Flavescens - Effect of Sophora Flavescens 0.5 g/L and N-Methylcytisine on CYP3A4 in HepaRG Cells Experiment - 2 (id=NPDI-COzHAQ)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
Cell system PXR-transfected hepatic cells
Results
| Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
|---|
Experimental Conditions
mRNA expression
2x10^5 cells/ml (100 μl in each well)
0.5 g/L
48 hours
10 . Sophora Flavescens - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 6 (id=NPDI-WjNEBg)
In Vitro Nuclear Receptor Induction Experiment
Induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
11 . Allomatrine - Effect on PXR Activation Experiment - 7 (id=NPDI-VDv5UA)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
12 . Allomatrine - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 5 (id=NPDI-N3gejQ)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
13 . Matrine - Effect on PXR Activation Experiment - 3 (id=NPDI-ytkNzA)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
14 . Oxymatrine - Effect on PXR Activation Experiment - 2 (id=NPDI-UIkeTg)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
15 . Oxymatrine - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 1 (id=NPDI-4_VbMg)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
16 . Sophocarpine - Effect on PXR Activation Experiment - 5 (id=NPDI-KG9M2g)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
17 . Sophocarpine - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 3 (id=NPDI-SFzJpg)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
18 . Sophoranol - Effect on PXR Activation Experiment - 6 (id=NPDI-vhDPDg)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours
19 . Sophoranol - Pretreatment of Sophora Flavescens and Constituents on CYP3A4 in DPX2 Cells Experiment - 4 (id=NPDI-cw3k7g)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
> control
- CYP3A4 4306811
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)
2x10^5 cells/ml (100 μl in each well)
10 μM
48 hours
20 . Tetrandrine - Effect on PXR Activation Experiment - 1 (id=NPDI-KccbZQ)
In Vitro Nuclear Receptor Induction Experiment
Non-induction was detected. Cutoff used —
≥ positive control (rifampicin)
- 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)
2x10^5 cells/ml (100 μl in each well)
10 μM
24 hours