”The MeOH extract exhibited significant inhibition of the major human CYP450 isozymes (CYP3A4, CYP1A2, CYP2D6, CYP2C9, and CYP2C19). The strongest inhibition was observed by the extract for CYP3A4 (IC50 1.7 ± 0.1 μg/mL) followed by CYP2C19 (IC50 4.0 ± 0.3 μg/mL). Among the tested phytochemicals, the most potent inhibitors were isovitexin on CYP3A4 (IC50 3.4 ± 0.2 μM), vitexin on CYP2C9 (IC50 8.0 ± 0.2 μM), and thermopsoside on CYP2C19 (IC50 9.5 ± 0.2 μM). The two major, structurally related compounds aspalathin and nothofagin exhibited a moderate pregnane-X receptor (PXR) activation, which was associated with increased mRNA expression of CYP3A4 and CYP1A2, respectively. These results indicate that a high intake of nutraceuticals containing rooibos extracts may pose a risk of herb–drug interactions when consumed concomitantly with clinical drugs that are substrates of CYP enzymes.”

https://pubs.acs.org/doi/abs/10.1021/acs.jafc.9b00846