- Natural product: Gou Teng (Uncaria rhynchophylla)
- Associated study: Identification of PXR activators from Uncaria rhynchophylla (Gou Teng)
In Vitro Enzyme Induction Experiment
Isocorynoxeine on CYP3A4 Activity
Induction was detected. Cutoff used —
Not available
- CYP3A4 4306811
Cell system DPX2 (HepG2 transfected with PXR)
Results
Sample | Compound measured | Value | Measurement | Study sequence | Additional information | N replicates |
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Experimental Conditions
Midazolam was utilized as a substrate for CYP3A4 activity assay (Olsen et al., 2016). Briefly, ~250,000 DPX2 cells were seeded on a 24-well plate and cultured for 24 h. After treatment with herbal extracts or chemicals for another 24 h, cells were washed with PBS. Midazolam (50 µM) in fresh medium was added and incubated for 2 h. Afterward, 100 µl medium was collected from each well, and mixed with 100 µl cold acetonitrile. The mixtures were centrifuged at 13,000 rpm for 15 min, and the supernatant was collected for analysis of 1'- OH-MDZ, a CYP3A4-mediated metabolite of midazolam.
Enzyme activity
~250,000 DPX2 cells were seeded on a 24-well plate
UPLC-QTOFMS