The effect of the candidate compounds against CYP3A4 activity was performed by P450-Glo™ CYP3A4 Assay (Luciferin-IPA) Cell-Based/Biochemical Assay (Promega). The expression of the CYP3A4 gene of HepG2 cells could be induced by 25 μM rifampicin. Cells were typically exposed for 24–72 h. The cells were then treated with various concentrations of test compounds for 72 h. Ketoconazole was used as the positive group. Finally, the P450-Glo™ CYP3A4 Assay (Luciferin-IPA) Cell-Based/Biochemical Assay (Promega) was added to pyrolysis, the treated HepG2 cells, and the fluorescence was detected by SoftMax Pro 6.1 (Beckman counter). The relative CYP3A4 activity was estimated as the formula: (the fluorescence of YS-7a treated/YS-7a treated HepG2 cells)/(the fluorescence of control/control HepG2 cells).
Quan X., Du H., Xu J., Hou X., Gong X., Wu Y., Zhou Y., Jiang J., Lu L., Yuan S., Yang X., Shi L, & Sun L. (2019). Novel Quinoline Compound Derivatives of NSC23925 as Potent Reversal Agents Against P-Glycoprotein-Mediated Multidrug Resistance. Frontiers in Chemistry, 7, 820.
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