In Vitro Enzyme Inhibition Experiment
Inhibition of UGT1A1, 1A8, and 1A10 by (-)-Epicatechin Gallate (Ki determination)
Inhibition was detected. Cutoff used — Not provided
- UGT1A1 40782950
Cell fraction Pooled human intestinal microsomes -7999663
The precipitant used was (-)-epicatechin gallate. Information regarding enzymes involved in the formation of raloxifene metabolites was obtained from Gufford et al., 2015 (Drug Metab Dispos. 2015 Sep;43(9):1353-9).
Using methods 1 and 2 provided by the authors, enterocyte concentrations for (-)-epicatechin gallate were estimated to be 8.5 and 0.29 µM, respectively, after administration of one bag of T21 green tea. With the Ki value of approximately 1 µM, the corresponding AUCi/AUC ratios were predicted to be 6.5 and 1.3, respectively.
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