Safety Assessment of Phytochemicals Derived from the Globalized South African Rooibos Tea (Aspalathus linearis) through Interaction with CYP, PXR, and P-gp

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.