Table 2.
Enzyme | RDI of Pterostilbene (mg) | IC50 (µM) | V/D index (L/dose) |
---|---|---|---|
CYP2C8 | 250 | 26.9 ± 5.6 | 36.30 |
CYP3A4 | 250 | >100 | 4.70 |
UGT1A1 | 250 | >500 | <2 |
UGT1A6 | 250 | 26.7 ± 40.7 | 36.50 |
UGT1A9 | 250 | >100 | 3.89 |
UGT1A8/10 | 250 | 92.7 ± 18.4 | 10.53 |
Enzyme selective substrates and pooled HLM or HIM were incubated with at least four different concentrations of pterostilbene. All incubations were performed in duplicate. Using nonlinear regression, rough IC50 values were calculated by fitting the IC50 equation to percent of activity remaining (Material and Methods-Data analysis). Values are reported as best fit IC50 (mean ± standard error). All resulting values had r2 value for goodness of fit of at least 0.9. Volume per dose index (VDI) values were calculated as mentioned in materials and methods. The recommended daily intake values were determined based on the commercially available products and a previous clinical study (Riche, 2012).